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DNA-RNA Transcription Regulators

STAT3 Signaling Pathway
Signal Transducers and Activators of Transcription (STATs) are transcription factors that are phosphorylated by JAK kinases in response to cytokine activation. Upon activation, the STATs dimerize and are localized to the nucleus where they activate transcription of cytokine-responsive genes. There are at least three JAK kinases and at least six distinct STAT proteins involved in this complex signaling pathway. Cytokines that activate STAT3 include growth hormone, IL-6 family cytokines, and G-CSF. STAT3, as well as STAT5, induces progression through the cell cycle, prevents apoptosis and upregulates oncogenes, such as c-myc and bcl-x and may play a role in oncogenesis. STAT3 has been shown to play a critical role in hematopoiesis. The importance of STAT3 is underscored by the failure of mice lacking STAT3 to survive embryogenesis. Crosstalk from pathways other than JAK kinases also leads to phosphorylation and activation of STAT3 as indicated by a role of mTOR (mammalian target of rapamycin, or p70 S6 kinase) and MAP kinase pathways in STAT3 activation and signaling.

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SML0962 M-110 ≥98% (HPLC) M-110 is a highly isoform-selective, cell permeable and potent ATP-competitive inhibitor of the PIM kinase family that prefers PIM-3. M-110 is an inhibitor of Wnt/β-catenin signaling that act downstream of the symb-catenin destruction complex to inhibit both Wnt-induced and cancer associated constitutive Wnt signaling via destabilization of β-catenin. The compound chelates iron in vitro and in intact cells. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM, with no activity on normal human peripheral blood mononuclear cells up to 40 μM.
SML1565 A-196 ≥98% (HPLC) A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines. For full characterization details, please visit the A-196 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML0570 21H7 ≥98% (HPLC) 21H7 is an inhibitor of Wnt/β-catenin signaling that act downstream of the symb-catenin destruction complex to inhibit both Wnt-induced and cancer associated constitutive Wnt signaling via destabilization of β-catenin. The compound chelates iron in vitro and in intact cells. 21H7 decrease the viability of mouse B-lymphoma W10 cells, with LD50 values of 0.4 to 1.0 μM, while is significantly less cytotoxic to normal cells.
SML1410 A-366 ≥98% (HPLC) A-366 is an SGC chemical probe for G9a/GLP, developed in collaboration with Abbvie. A-366 is a potent, selective inhibitor of the histone methyltransferase G9a. The IC50 values for G9a inhbition in enzymatic and cell based assays are 3.3 and approximately 3 μM, respectively. A-366 has little or no detectable activity against a panel of 21 other methyltransferases. For full characterization details, please visit the A-366 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1879 A-395N ≥98% (HPLC) New A-395N is a control probe for A-395, which is a chemical probe for polycomb protein EED. A-395 is a potent and selective chemical probe for the polycomb protein EED (embryonic ectoderm development), an essential component of Polycomb repressive complex 2 (PRC2), involved in transcriptional repression through methylation of histone H3K27. A-395N is structurally similar, but exhibits no activity in the biochemical and cellular assays, so is an ideal control compound.
SML1775 K-756 ≥98% (HPLC) K-756 is an orally available, potent and selective tankyrase inhibitor, which binds to the induced-pocket of tankyrase. K-756 is a selective Wnt/β-catenin pathway inhibitor that stabilizes Axin and reduces active β-catenin. K-756 inhibits the proliferation of APC mutant colorectal cancer COLO 320DM and SW403 cell lines.
475956 c-Myc Inhibitor - CAS 403811-55-2 - Calbiochem The c-Myc Inhibitor, also referenced under CAS 403811-55-2, controls the biological activity of c-Myc.  
475957 c-Myc Inhibitor II - CAS 413611-93-5 - Calbiochem The c-Myc Inhibitor II, also referenced under CAS 413611-93-5, controls the biological activity of c-Myc.  
475965 c-Myc Inhibitor III, Mycro2 - Calbiochem The c-Myc Inhibitor III, Mycro2 controls the biological activity of c-Myc.  
480404 NFAT Inhibitor, MCV1 - Calbiochem The NFAT Inhibitor, MCV1 controls the biological activity of NFAT.  
SML0357 AcH4-21 trifluoroacetate salt ≥95% (HPLC) AcH4-21 is a good substrate of Protein Arginine Methyltransferases (PRMTs).
A1410 Actinomycin D from Streptomyces sp., ~98% (HPLC) Actinomycin D inhibits the proliferation of cells by forming a stable complex with double-stranded DNA, inhibiting DNA-primed RNA synthesis and causing single-stranded breaks in DNA. It has been shown to be an inhibitor of the minus-strand transfer step in reverse transcriptase.
A9415 Actinomycin D from Streptomyces sp., suitable for cell culture, ≥95% Actinomycin D inhibits the proliferation of cells by forming a stable complex with double-stranded DNA, inhibiting DNA-primed RNA synthesis and causing single-stranded breaks in DNA. It has been shown to be an inhibitor of the minus-strand transfer step in reverse transcriptase.
A4262 Actinomycin D from Streptomyces sp., ≥95% (HPLC) Actinomycin D inhibits the proliferation of cells by forming a stable complex with double-stranded DNA, inhibiting DNA-primed RNA synthesis and causing single-stranded breaks in DNA. It has been shown to be an inhibitor of the minus-strand transfer step in reverse transcriptase.
SML0839 AGI-5198 ≥98% (HPLC) AGI-5198 is a highly potent and selective mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.
SML0895 AGI-6780 ≥98% (HPLC) AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2. Several human cancers have somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2), confering a gain-of-function in cancer cells in which the mutant enzymes produce the oncometabolite (R)-2-hydroxyglutarate, [(R)-2HG]. (R)-2HG inhibits histone- and DNA-modifying enzymes, resulting in altered gene expression, histone and DNA hypermethylation, and inducing a block in cellular differentiation that promotes tumorigenesis. AGI-6780 reduced (R)-2HG levels in cell lines overexpressing IDH2/R140Q with an EC50 of 20 nM, and induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. AGI-6780 binds allosterically at the dimer interface of IDH2. AGI-6780 shows good selectivity against other dehydrogenases, including the closely related IDH1-WT or R132H mutant enzymes.
A8231 AGK2 ≥97% (HPLC), powder AGK2 is a SIRT2 inhibitor. AGK2 rescues dopamine neurons from α-synuclein toxicity in Parkinson′s disease models. IC50 for SIRT2 = 3.5 uM. AGK2 is >15-fold more selective for SIRT2 than SIRT1 and SIRT3. AGK2 may be the most selective SIRT2 inhibitor available.
SML1344 AK-1 ≥98% (HPLC) AK-1 is a cell permeable, potent and specific SIRT2 inhibitor that induced proteasomal degradation of the Snail transcription factor.
A2263 α-Amanitin from Amanita phalloides, ≥90% (HPLC), powder The major toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but does not inhibit RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.
A1304 β-Amanitin from Amanita phalloides ~90% (HPLC) Toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but not RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.
A8100 β-Amanitin–poly-L-lysine bound ≥85% Toxic constituent of the mushroom, Amanita phalloides, inhibits eukaryotic RNA polymerase II and III, but not RNA polymerase I or bacterial RNA polymerase. Inhibits mammalian protein synthesis.
SML0628 8-Aminoadenosine ≥98% (HPLC) 8-Aminoadenosine, a ribose nucleoside, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine also inhibits transcription and polyadenylation. 8-Aminoadenosine potently inhibits varies breast cancer cell lines proliferation and activates cell death independent of p53. 8-NH2-Ado is highly cytotoxic to other cancer cell lines.
A8236 AN-9 ≥95% (HPLC) HDAC Inhibitor tested as an anti-cancer drug; butyric acid pro-drug
A7236 Anacardic acid Anacardic acid is a HAT (Histone Acetyltransferase) inhibitor.
A8851 Apicidin ≥98% (HPLC), from microbial Apicidin is a cyclic tetrapeptide that inhibits histone deacetylase. Apicidin has antiproliferative activity on various cancer cell lines and HeLa cells, accompanied by cell arrest at the G1 phase. It has been shown to induce selective changes in the expression of p21 and gelsolin, induce apoptosis in HL60 cells, and exhibit antiprotozoal, antiparasitic, and potential antimalarial properties.
SML1906 AS1517499 ≥98% (HPLC) New AS1517499 is a potent STAT6 (signal transducer and activator of transcription 6) inhibitor (IC50 = 21 nM against IL-4-dependent reporter activity) that selectively prevents anti-CD3- & IL-4-induced T-helper cell 2 (Th2) differentiation of mouse spleen T cells (IC50 = 2.3 nM), without affecting anti-CD3- & IL-12-induced Th1 differentiation. AS1517499 in vivo effecicacy is demonstrated in various animal models of immunological disorders, including the autoimmune Graves’ disease, antigen-induced bronchial hypercontractility (10 mg/kg i.p.). AS1517499 treatment (10 mg/kg/day i.p.) following early gliomagenesis blockage by a CSF-1R inhibitor is also shown to greatly prolong the survival rate when compared with CSF-1R inhibition alone in a murine model of PDGF-driven glioma (PDG).
SML1692 AS8351 ≥98% (HPLC) AS8351 is an iron chelator that has been found to inhibit of histone demethylase KDM5B (JARID1B), a histone H3K4 demethylase involved in regulation of cell proliferation and stem cell self-renewal and differentiation. AS8351 is thought to inhibit KDM5B by competing with a-ketoglutarate for chelating iron that KDM5B requires as a co-factor.
B4061 BATCP ≥98% (HPLC), solid HDAC 6 selective substrate (over HDAC 1, Class II over Class I).
SML1780 BAY-588 ≥98% (HPLC) BAY-588 is an inactive control probe for BAY-876 (catalog no. SML1774). BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. For characterization details of BAY-876 and BAY-588, please visit the BAY-876 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
SML1603 BAY-598 ≥98% (HPLC) BAY-598 is a potent, peptide-competitive chemical probe for SET and MYND domain-containing protein 2 (SMYD2), a lysine methyl transferase inhibitor that dimethylates histone H3K36 and methylates histone H3K4. SMYD2 also methylates Lys-370 of p53, leading to decreased DNA-binding activity. SMYD2 is over-expressed in several cancers with poor prognosis. BAY-598 inhibits in vitro methylation of p53K370 with an IC50 value of 27 nM and in cells with an IC50 value < 1 μM. BAY-598 is more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. BAY-598 can be used with in vivo experiments. For full characterization details, please visit the BAY-598 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1774 BAY-876 ≥98% (HPLC) BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. It had an IC50 value of 2 nM in vitro and inhibited glucose uptake by Hela-MaTu cells with an IC50 value of 3.2 nM. BAY-876 was at least 130-fold selective for GLUT1 relative to GLUT2, GLUT3, GLUT4 and a panel of 18 kinases and 68 proteins. For full characterization details, please visit the BAY-876 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc
SML1817 BCI-121 ≥98% (HPLC) BCI-121 is a substrate-competitive SMYD3 inhibitor that reduces nuclear histone H3 lys4 di- and tri-methylation level (by 50%/H3K4me2 and 40%H3K4me3 in HT29 cells; 100 μM BCI-121 for 48 h), downregulates known SMYD3 target genes transcription, and selectively affects SMYD3-dependent proliferation of cancer cultures (46%/HT29 and 54%/HCT116 proliferation reduction; 100 μM BCI-121 for 72 h) with little antiproliferation efficacy toward low SMYD3-expressing cancer cells. BCI-121 targets SMYD3 via direct affinity interaction (kon 357.7/M/s; koff 4.23×10-3/s; KD=koff/kon = 11.8 μM) and effectively competes against histone for SMYD3 binding (%inhibition/[histone H4 peptide]:[BCI-121] ratio = 36.5%/1:1 and 51.0%/1:2.5).
SML0867 BG45 ≥98% (HPLC) BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM) over HDAC1, 2. BG45 did not inihibit HDAC6. BG45 signigicantly inhibited tumor growth in a mouse model of multiple myeloma either alone and synergistically in combination with bortezomib.
B9311 BIX 01294 trihydrochloride hydrate ≥98% (HPLC), powder BIX 01294 is a selective histone methyl transferase inhibitor. In its inhibition of the histone lysine methyltransferases, BIX 01294 does not compete with cofactor S-adenosyl-methionine. The target enzyme is G9a, and it selectively impairs G9a HMTase and the generation of H3K9me2 in vitro.
B5313 BIX-01338 hydrate ≥98% (HPLC) BIX-01338 is a non-selective histone lysine methyltransferase inhibitor.
SML1183 BMH-21 ≥98% (HPLC) BMH-21 is a potent inhibitor of RNA Pol I. BMH-21 binds strongly to GC-rich DNA sequences, ultimately inhibiting RNA Pol I, blocking transcription and disrupting the nucleolar structure. BMH-1 causes dissociation of the RPA194 catalytic subunit from Pol I, and disassembly of Pol I:DNA complexes. The compound BMH-21 inhibits proliferation of a broad range of tumor cell lines.
B8063 BML-210 ≥98% (HPLC), powder BML-210 is a histone deacetylase inhibitor. Treatment of A549 cells with BML-210 results in a dose-dependent increase in acetylated histone levels (EC50 = 36 μM). In HeLa extracts, the IC50 for inhibition of HDAC activity is 80 μM.
SML1639 BRD3308 ≥98% (HPLC) BRD3308 is a highly selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 value of 65 nM for HDAC3 vs. IC50 values of 1.08 μM and 1.15 μM for HDAC1 and HDAC2, respectively. BRD3308 protected pancreatic β cells, suppressing inflammatory cytokine-induced apoptosis and increasing insulin release without the toxicity associated with HDAC1 and HDAC2 inhibitors. In a rat model of type 2 diabetes, BRD3308 reduced hyperglycemia and increased insulin secretion without affecting weight gain. In another study, BRD3308 was found to activate HIV-1 transcription, disrupting HIV-1 latency.
SML0567 BRD4770 ≥98% (HPLC) BRD4770 is a selective inhibitor of the histone methyltransferase G9a. BRD4770 blocks lysine residue 9 methylation of histone H3 without inducing apoptosis. In PANC-1 cells, BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway, induces senescence and inhibits anchorage-dependent and -independent growth.
SML1361 BRD73954 ≥98% (HPLC) BRD73954 is the first discovered histone deacetylase 6/8 dual inhibitor. BRD73954 has an IC50 of 36 nM for the class IIb HDAC6 and 120 nM for the class I HDAC8 with IC450′s ranging from 9 μM to greater than 33 μM for other HDACs.
SML0575 BRD9539 ≥98% (HPLC) BRD9539 is a very specific inhibitor of the enzymatic activity of histone methyltransferase G9a. The compound has poor activity in cell based assays.
SML0878 BRD9757 ≥98% (HPLC) BRD9757 is a selective inhbitor of the histone deacetylase HDAC6 (IC50 = 30 nM). BRD9757 dose dependently increases levels of acetylated α-tubulin in HeLa cells, with no affect on H3 acetylation.
SML0113 Brequinar sodium salt hydrate ≥97% (HPLC) Brequinar exhibits anti-neoplastic activity against refractory solid tumors in human and mouse models. Continuous treatment is required for depletion of pyrimidine pools in the cancer cells and tumor inhibition.
Brequinar inhibits dihydroorotate dehydrogenase (DHODH), the fourth enzyme in the de novo pyrimidine biosynthesis pathway, preventing the synthesis of DNA and RNA. Brequinar has recently been found to have antiviral activity against a broad spectrum of viruses including flaviviruses (dengue virus, West Nile virus, yellow fever virus, and Powassan virus) and also a plus-strand RNA alphavirus (Western equine encephalitis virus) and a negative-strand RNA rhabdovirus (vesicular stomatitis virus).
SML1078 4-Bromo-Resveratrol ≥98% (HPLC) 4-Bromo-Resveratrol is a resveratrol analog that potently inhibits Sirt1 and Sirt3.
SML0027 Butyrylhydroxamic acid ≥98% (HPLC) Butyryl hydroxamic acid is a cell permeable HDAC inhibitor. Butyryl hydroxamic acid has similar potency against class I HDAC family members as 4-Phenylbutyryl hydroxamic acid (SML0026), but is approximately 5-10 fold less potent against class IIa enzymes than 4-Phenylbutyryl hydroxamic acid.
SML0002 C646 ≥98% (HPLC) C646 is a competitive histone acetyltransferase (HAT) p300/CBP inhibitor with a Ki of 400 nM and is selective versus other acetyltransferases.
C646 is a potent, cell permeable and selective inhibitor of p300 and CBP (p300/CBP) histone acetyltransferases. Inhibition of p300/CBP by C646 affects the activity of a variety of transcriptional factors such as NF-κB, p53 and MyoD that are associated with physiology, disease processes, hippocampal synaptic plasticity, spatial memory and contextual fear.
SML0653 Capecitabine ≥98% (HPLC) Capecitabine is an anti-cancer drug, a prodrug of doxifluridine, metabolized to 5-fluorouracil at the tumor site. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5′-Deoxy-5-fluorocytidine (5′-DFCR) and 5′-Deoxy-5-fluorouridine (5′-DFUR), to form 5-fluorouracil.
SML1281 Capecitabine Ready Made Solution 10 mg/mL in DMSO Capecitabine is a fluoropyrimidine carbamate that undergoes preferential conversion to 5-fluorouracil in cancerous tissues.
Capecitabine is an anti-cancer drug, a prodrug of doxifluridine, metabolized to 5-fluorouracil at the tumor site. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5′-Deoxy-5-fluorocytidine (5′-DFCR) and 5′-Deoxy-5-fluorouridine (5′-DFUR), to form 5-fluorouracil.
SML0458 Cardionogen-1 ≥98% (HPLC) Cardionogen-1 is cardiomyocyte promoter and an inhibitor of Wnt/β-catenin dependent transcriptional activity with an EC50 of 23 nM in murine stem cells and zebrafish embryos. It induces cardiac cell formation in both murine stem cells and zebrafish embryos, expanding cardiac progenitor cells.
SML0427 Cardionogen-2 ≥98% (HPLC) Cardionogen-2 is a biphasic modulator of cardiogenesis that enlarges the size of the zebrafish embryonic heart by promoting cardiomyocyte formation. Also, cardionogen-2 promotes murine ES cells to differentiate into beating cardiomyocytes. Apparently, cardionogen-2 inhibits Wnt/b-catenin dependent transcriptional activity. Treatment of zebrafish embryos with cardionogen-2 significantly enlarged both the atrium and ventricle, without causing apparent defects of embryonic morphology or other organ development.
C1494 Carmofur ≥98% (HPLC), powder Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent.
SML1399 CCT031374 hydrobromide ≥98% (HPLC) CCT031374 is an inhibitor of TCF-dependent transcription. CCT031374 is a selective β-catenin signaling inhibitor that decreases the intracellular/soluble β-cat level. CCT031374 inhibits  proliferation of numberous cancer cell lines by induction of apoptosis.
SML0151 CCT036477 ≥98% (HPLC) CCT036477 is an inhibitor of Wnt signaling. It does not alter β-catenin levels but blocks transcription at the β-catenin level. CCT036477 inhibited growth in several cancer cell lines and showed clear activity in vivo, blocking development of Zebrafish and Xenopus embryos and expression of Wnt target genes.
C9623 Chetomin from Chaetomium cochliodes, ≥98% (HPLC) Chetomin is a natural metabolite produced by several species of the genus Chaetomium. Chetomin is an epidithiodioxopiperazine known to disrupt the hypoxia-inducible factor (HIF) pathway. Chetomin blocks the interaction of HIF1α and HIF2α with transcriptional co-activators p300 and cAMP response element binding (CREB) binding protein (CBP), thereby attenuating hypoxia-inducible transcription. Disrupting the ability of tumors to adapt to hypoxia leads to decreased tumor growth and can serve as an antitumor stratagy. Chetomin also suppresses the proliferation of LPS-induced mouse spleen lymphocytes.
Chetomin is a natural metabolite produced by several species of the genus Chaetomium. Chetomin disrupts the hypoxia-inducible factor (HIF) pathway, blockomg the interaction of HIF1α and HIF2α with transcriptional co-activators p300 and cAMP response element binding (CREB) binding protein (CBP), thereby attenuating hypoxia-inducible transcription. Disrupting the ability of tumors to adapt to hypoxia leads to decreased tumor growth; hypoxia can also promote resistance to radiotherapeutics. By both of these mechanisms, chetomin shows promise as a lead compound in antitumor research. Chetomin also suppresses the proliferation of LPS-induced mouse spleen lymphocytes.
C8742 CHIC-35 ≥97% (chiral, HPLC) CHIC-35 is cell-permeable, metabolically stable, and very potent inhibitor of SIRT1; IC50 of S-isomer is 60 nM; IC50 of mixed isomers is 124 nM. There is no inhibition of SIRT3 or HDAC. The IC50 for SIRT2 is 2.77 μM. Sirtuins are protein deacetylases, which represent a new class of histone deacetylases (HDAC) involved in gene silencing. SIRT modulators are potential therapeutics for cancer, diabetes, muscle differentiation, heart failure, neurodegeneration, and aging.
SML0487 CID 2818500 ≥98% (HPLC) CID 2818500 (trans-α-Nitrostilbene; 1,1′-[(1Z)-1-Nitro-1,2-ethenediyl]bis-benzene) is a selective inhibitor of Protein Arginine Methyltransferases PRMT1 and PRMT8. PRMT1 is responsible for the majority of arginine methylation in the cell involved in transcription, chromatin modification, and signal transduction. CID 2818500 has an IC50 values of 11 μM for PRMT1, and does not inhibit PRMTs 3, 4, and 6, although it does inhibit PRMT8. The mechanism is believed to involve a specific S-adenosylmethionine (SAM)-binding cysteine present only in the Type I PRMTs PRMT1 and PRMT8 and absent in other SAM-dependent methyltransferases.
SML0634 CID2858522 ≥98% (HPLC) CID2858522 specifically inhibits NF-kB activation downstream of protein kinsase C (PKC). CID2858522 dose dependently inhibits NF-kB reporter activity in PMA-ionomycin stimulated HEK293 cells, but does not affect NF-kB activity in cells challenged with TNFa, retinoic acid, or stimulation of the toll-like receptor signaling pathway.
SML0516 CID 5380390 ≥98% (HPLC) CID 5380390 (trans-2,3-Dimethoxy-ß-nitrostyrene) is a selective inhibitor of Protein Arginine Methyltransferases PRMT1 and PRMT8. PRMT1 is responsible for the majority of arginine methylation in the cell involved in transcription, chromatin modification, and signal transduction. CID 5380390 has an IC50 values of 23 μM for PRMT1, and does not inhibit PRMTs 3, 4, and 6, although it does inhibit PRMT8. The mechanism is believed to involve a specific S-adenosylmethionine (SAM)-binding cysteine present only in the Type I PRMTs PRMT1 and PRMT8 and absent in other SAM-dependent methyltransferases.
PZ0130 CP-64434 hydrate ≥98% (HPLC) CP-064434 is an antibiotic; anti-proliferative HDAC inhibitor.
SML1212 CPI203 ≥98% (HPLC) CPI203 is an inhibitor of BRD4, a bromodomain-containing protein that binds to histones to regulate recruitment of transcription factors. BRD4 is also an RNA Pol II kinase. CPI203 blocks BRD4 kinase activity in cells and in vivo. It has shown synergistic antitumor activity with lenalidomide in bortezomib-resistant mantle cell lymphoma.
C9873 CPTH2 ≥98% (HPLC), powder CPTH2 is a histone acetyltransferase (HAT) inhibitor modulating the Gcn5 network. Histone Acetyltransferase (HAT) inhibitor modulating Gcn5 network. Histone acetyltransferases (HATs) act as transcriptional coactivators. Histone acetylation plays an important role in regulating the chromatin structure and is tightly regulated by two classes of enzyme, histone acetyltransferases (HAT) and histone deacetylases (HDAC). Deregulated HAT and HDAC activity plays a role in the development of a range of cancers. Consequently, inhibitors of these enzymes have potential as anticancer agents.
C5624 Cryptotanshinone ≥98% (HPLC) Cryptotanshinone is a quinoid diterpene isolated from the root of the Asian medicinal plant, Salvia miotiorrhiza bunge. Recently it was discovered that the compound is a potent STAT3 inhibitor. Cryptotanshinone rapidly inhibited STAT3 Tyr705 phosphorylation through a JAK2-independent mechanism. Cryptotanshinone selectively inhibits STAT3-activated cell lines through binding to monomer STAT3, subsequently blocking the dimerization and inhibiting STAT3 transcriptional regulatory activity. Previously, it was reported that the compound counteracts inflammation through the inhibition of cyclooxygenase II activity and endothelin-1 expression. In traditional oriental medicine dried roots of Salvia Miltiorrhiza Bunge (Danshen) have commonly been used for the treatment of circulatory disorders, liver disease, coronary heart disease, hepatitis, and chronic renal failure.
SML0597 Daurisoline ≥98% (HPLC) Daurisoline alkaloid isolated from the rhizomes of Menispermum dauricum that exhibit varies pharmacological activities including antiplatelet aggregation, anti-inflammatory, neuron-protective properties, and antiarrhythmic effect. It appears that antiarrhythmic effect of daurisoline is maintained through blockade of hERG channels.
Daurisoline is antiarrythmic, anti-inflammatory, neuron-protective; and blocks hERG channels.
SML1512 DC_05 ≥98% (HPLC) DC_05 is a potent and selective non-nucleoside DNMT1 (DNA methyltransferase 1) inhibitor that significantly inhibits cancer cell proliferation.
SML0305 3-Deazaneplanocin A hydrochloride ≥97% (HPLC) 3-Deazaneplanocin A (DZNep) is an S-Adenosylhomocysteine Hydrolase inhibitor and histone methyltransferase EZH2 inhibitor. It switches on repressed tumor suppressor genes and induces apoptosis by inhibiting the expression of EZH2.
SML1627 DFHBI DFHBI is a membrane permeable and nontoxic fluorogen, which produces fluorescence upon binding. RNA aptamers Spinach, Spinach2 and Broccoli. DFHBI displays fluorescence excitation maxima of 447 nm and peak fluorescence emission of 501 nm. DFHBI is used for imaging RNA in cells.
D1916 5,6-Dichlorobenzimidazole 1-β-D-ribofuranoside Inhibitor of RNA synthesis; causes premature termination of transcription. CK2 (casein kinase-2) inhibitor.
D2629 6-(Dimethylamino)purine ≥98%  
D6071 Diphenylacetohydroxamic acid ≥98% (HPLC) Diphenylacetohydroxamic acid is a class IIa selective histone deacetylase inhibitor.
SML1724 Displurigen ≥98% (HPLC) Displurigen is a cell-permeable, phenylthiochromen-4-one derived compound that disrupts the pluripotency of human embryonic stem cells by targeting HSPA8/HSC70 and affects its binding to Oct4. Inhibits ATPase activity of HSP70 (IC50 = 225 μM). Displurigen has shown to diminish the mRNA levels of Oct4 and Nanog within 24 hours of treatment and causes a complete annihilation of OCT4+  and NANOG+  bearing cells within 4 days of treatment (~ 10 μM). It does not induce apoptosis and has no significant effect on cell cycle progression.
D3695 DMOG ≥98% (HPLC) DMOG is a cell permeable prolyl-4-hydroxylase inhibitor, which upregulates HIF (hypoxia-inducible factor). The protein level of HIF-1α subunit is post-transcriptionally regulated by prolyl and asparaginyl hydroxylase (PAH). Suppression of PAH activity increases endogenous HIF-1α levels. DMOG is a cell permeable, competitive inhibitor of prolyl hydroxylase domain-containing proteins (PHDs and HIF-PHs). It has been discovered that the DMOG posseses neuroprotective effect on NFG deprived cell cultures through preservation of glucose metabolism. DMOG also attenuates myocardial injury in a rabbit ischemia reperfusion model. DMOG is more potent than the older inhibitor 4-Phenyl-pyridine-2,5-dicarboxylic acid (R395889; Sigma-Aldrich rare chemicals library). The IC50 is 5.18 μM.
D4071 5, 15-DPP 5, 15-DPP is a selective STAT3 inhibitor and a selective STAT3-SH2 antagonist
D6321 Droxinostat ≥98% (HPLC) Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8.
SML1516 DS-437 ≥98% (HPLC) DS-437 is an analog of S-adenosyl methionine (SAM ), which inhibits protein arginine methyltransferases PRMT5 and PRMT7 (IC50 5.9 and 6 μM) with little interaction against a panel of 30 other human methyltransferases.
E8534 E3330 ≥98% (HPLC) E3330 is a specific inhibitor of AP endonuclease 1 redox domain. E3330 inhibits APE-1 regulation of transcription factors, but does not affect Ape1 DNA repair activity. AP endonuclease 1 (APE1; also known as REF-1) is a multifunctional protein with dual functions in DNA repair and redox regulation of transcription factors. It is involved in apurinic/apyrimidinic endonuclease DNA base excision repair activity, in proofreading exonuclease activity, and in modulating DNA binding activity of several transcription factors including NF-κB, Egr-1, p53, AP-1, CREB, HIF-α, and members of the Pax family. APE1 is overexpressed in several human cancers, and disruption of APE1 function has detrimental effects on cancer cell viability. E3330 significantly reduces the growth of human pancreatic cancer cells in vitro and inhibits pancreatic cancer cell migration.
SML0477 Echinomycin ≥98% (HPLC) Echinomycin is an antitumor antibiotic and potent hypoxia inducible factor 1α (HIF-1α) inhibitor. It binds to DNA via bifunctional intercalation, blocking the binding of HIF-1α, a transcription factor important in tumor growth. Echinomycin selectively eliminated cancer stem cells in a study with mouse lymphoma and human AML xenogeneic models, eradicating the lymphomas. Recently, echinomycin was also found to act as an antibiotic adjuvant having synergistic effects with novobiocin in gram negative bacteria.
E4143 (−)-Epigallocatechin gallate ≥95% Antioxidant polyphenol flavonoid that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors. ECGG inhibits fatty acid synthase and glutamate dehydrogenase activity.
E4268 (−)-Epigallocatechin gallate ≥80% (HPLC), from green tea Catechins are a plant derived polyphenolic anti-oxidants with phytotoxic properties. Racemic catechin may be used in studies on seed germination and plant invasiveness. Catechin and Epigallocatechin gallate (EGCG) may be used with other polyphenol flavonoids to study their effects in oxidation and peroxidation-related processes.
SML1421 EPZ015666 ≥98% (HPLC) EPZ015666 (GSK3235025) is a protein arginine methyltransferase PRMT5 inhibitor with an IC50 value of of 22 nM in biochemical assays and no inhibition up to the maximum tested concentration of 50 μM against a panel of 20 other protein methyltransferases. Inhibition was uncompetitive with respect to SAM. EPZ015666 showed dose-dependent antitumor activity in multiple in vitro and in vivo mantle cell lymphoma (MCL) models with treatment of MCL cell lines leading to inhibition of SmD3 methylation and cell death.
E7034 EX-527 ≥98% (HPLC) EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive.
SAB4200437 Anti-EXOSC1 antibody produced in rabbit ~1.0 mg/mL, affinity isolated antibody The exosome complex facilitates the splicing and degradation of mRNAs and non-coding RNAs. It is also essential for epigenetic gene regulation. It endogenously suppresses erythroid maturation. Within the complex, Exosc1 (exosome component 1) associates with Exosc6 to stabilize the complex. The binding of Exosc10 to Exosc1, Exosc6, and Exosc8 enhances the activity of the complex and positions Exosc1 for RNA binding.
SAB4200438 Anti-EXOSC5 (C-terminal) antibody produced in rabbit ~1.0 mg/mL, affinity isolated antibody  
SAB4200439 Anti-EXOSC5 (N-terminal) antibody produced in rabbit ~1.0 mg/mL, affinity isolated antibody  
SML0681 Febrifugine dihydrochloride ≥95% (HPLC) Febrifugine is an antimalarial, the active component of the Chinese herb Chang Shan. Recent studies indicate that its mechanism of action is as an inhibitor of prolyl-transfer RNA synthetase (ProRS).
SML1489 FICZ ≥95% (HPLC) FICZ is a potent high affinity ligand of the aryl hydrocarbon receptor (AhR), which is a ligand-activated transcription factor that activates the expression of aromatic hydrocarbon metabolizing enzyme genes such as the CYP1A1 gene and has also been shown to have multiple additional roles in cell-cycle regulation, development and maturation of many tissues, control of inflammation, and immune response. FICZ is a photoproduct of tryptophan and is believed to be an endogenous AhR ligand. It is extremely potent, with a Kd value of 0.07 nM.
PZ0030 Filibuvir ≥98% (HPLC) Filibuvir is an orally available, potent and selective inhibitor of the hepatitis C virus (HCV) nonstructural 5B (NS5B) RNA-dependent RNA polymerase that exhibits potent antiviral activity against subgenomic HCV replicons in cell culture assays. Also, Filibuvir potently inhibits viral replication in infected patients. Filibuvir interacts with the thumb site II of the viral polymerase.
F9057 FLLL31 ≥98% (HPLC) FLLL31 selectively binds to Janus kinase 2 and the STAT3 Src homology-2 (SH2) domain, effective inhibitors of STAT3 phosphorylation. STAT3 plays a critical role in early embryogenesis, but is largely dispensable in normal adult cells and tissues. On the other hand the JAK2/STAT3 signaling pathway is persistently activated in great number of human solid and blood cancers. Such activation is commonly associated with a worse prognosis. FLLL31 is a curcumin derivative locked in diketone-tautomeric form, which supposedly improves binding to SH2 domain. The compound inhibits JAK2 kinase activity and prevents STAT3 phosphorylation. FLLK31 is a potent and selective inhibitor of the STAT3 signaling pathway.
F5307 5−Fluoro−2′−deoxycytidine ≥98% (HPLC), powder 5-Fluoro-2′-deoxycytidine is a mechanism based DNMT (DNA cytosine-5 methyltransferase) inhibitor, that forms a covalent link with the cysteine residue in the active site of DNMT.
SML1162 5-Fluoro-1-propargyl-uracil ≥98% (HPLC) 5-Fluoro-1-propargyl-uracil is a biologically inert precursor, a prodrug that can be bioorthogonally activated to 5-fluorouracil iside a tumor that has a previously implanted palladium catalyst. Preliminary tests with pancreatic and colorectal cancer cells resulted in the death of than 80% of the malignant cells.
F8807 FM19G11 ≥98% (HPLC) FM19G11 is an inhibitor of Hypoxia Inducible Factors α (HIFα), reported to affect self-renewal and differentiation of stem cells. Hypoxia-inducible factors (HIFs) are transcription factors that respond to changes in available oxygen in the cellular environment. Among other functions (like angiogenesis), HIFα proteins affect the self-renewal and the differentiation processes of stem cells. FM19G11 inhibits the HIFα proteins that repress the target genes of the two α subunits, in various tumor cell lines as well as in adult and embryonic stem cell (ESC) models.
SML0413 FQI1 ≥98% (HPLC) FQI1 inhibits the DNA-binding activity of LSF, a ubiquitous transcription factor that is up regulated in many hepatocellular carcinomas (HCC). FQI1 inhibits LSF-dependent luciferase reporter expression, blocks proliferation in cancer cell lines, and induces apoptosis in liver cancer cells but is not toxic to primary hepatocytes. FQI1 also inhibits tumor growth in a mouse HCC xenograft model.
SML1481 FzM1 ≥98% (HPLC) FzM1 is an allosteric ligand of the Frizzled4 (Fz4) receptor and a Wnt/β-catenin pathway inhibitor, found by a screen for pharmacological chaperones for a misfolded mutant of the Frizzled4 (Fz4) receptor. FzM1 is believed to induce conformational changes in Fz4 by interacting with the third intracellular loop, ICL3, inhibiting binding of dishevelled (Dsh) and hampering the formation of the Fz4-Dsh complex that is necessary for β-catenin nuclear transport and ultimately transcription of TCF/LEF-regulated genes. FzM1 was tested on two tumor cell lines. U87MG glioblastoma cells acquired a more differentiated phenotype on application. FzM1 and FzM1alk also sped up the differentiation of Caco-2 cells. FzM1 has a log EC50 value of 5.74 for inhibition of Wnt antagonism.
SML1772 Givinostat hydrochloride hydrate ≥95% (HPLC) Givinostat (ITF2357) is a hydroxamate HDAC inhibitor that inhibits class I and class II enzymes. Givinostat posseses a very promising activity profile in multiple myeloma and acute myelogenous leukemia in vitro and in vivo. Givinostat also has anti-inflammatory activity and inhibits the secretion of the tumor necrosis factor-alpha (TNF-α), IL-1, and IL-6. Givinostat has been in multiple Phase 2 studies for both inflammatory diseases (Duchenne Muscular Dystrophy , Juvenile arthritis, Polycythemia Vera) and blood cancers (myelomas and lymphomas).
SML1878 GNF-1331 ≥98% (HPLC) New GNF-1331 is an orally available, potent and selective Porcupine (PORCN) inhibitor.
SML1251 Gomisin A ≥98% (HPLC) Gomisin A is a major dibenzocyclooctadiene lignan from medicinal plant Schizandra Chinese that exhibit a wide variety of interesting biological activities, including hepatoprotective, antiviral, anticancer, neuroprotective and anti-inflammatory. Gomisin A suppressed the expressions of iNOS and COX-2 in LPS-stimulated N9 microglia through suppression of NF-κB/MAPKs pathway.
SML0766 GSK343 ≥98% (HPLC) GSK343 is a potent, specific inhibitor of the histone H3-lysine 27 (H3K27) methyltransferase EZH2. GSK343 inhibits EZH2 enzymatic activity with an IC50 of 4 nM. The compound displays 60 fold selectivity for EZH2 vs. EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. The IC50 for inhibition of H3K27 methylation is < 200 nM in HCC1806 cells. For full characterization details, please visit the GSK343 probe summary on the Structural Genomics Consortium (SGC) website.

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SML1658 GSK484 ≥98% (HPLC) GSK484 is a potent selective reversible inhibitor of protein arginine deiminase PAD4, an enzyme believed to play a role in granulocyte and macrophage development leading to inflammation and immune response, and overexpressed in many tumors. GSK484 has IC50 values of 50 nM without calcium and 250 nM in the presence of 2 mM calcium. GSK484 showed minimal off-target activity tested against 50 other proteins with no activation across HDACs 1–11 even at 100 μM. GSK484 binds at a different site from the amidines, a conformation of the PAD4 active site where part of the site is reordered to form a β-hairpin. For full characterization details, please visit the GSK484 probe summary on the Structural Genomics Consortium (SGC) website.

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SML1751 GSK591 ≥97% (HPLC) GSK591 is a SGC probe for PRMT5. GSK591 is a potent and selective inhibitor of H4 histone methylation by PRMT5/MEP50 complex. For full characterization details, please visit the GSK591 probe summary on the Structural Genomics Consortium (SGC) website.

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SML0709 GSK-J1 ≥98% (HPLC) GSK-J1 is a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. For full characterization details, please visit the GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.

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SML0701 GSK-J4 ≥98% (HPLC) GSK-J4 is cell permeable prodrug rapidly hydrolysed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. The prodrug GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. For characterization details for GSK-J4 and full characterization details for GSK-J1, please visit the GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.

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SML1072 GSK-LSD1 ≥98% (HPLC) GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1). GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns. For full characterization details, please visit the GSK-LSD1 probe summary on the Structural Genomics Consortium (SGC) website.

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SML0456 HBB2 ≥98% (HPLC) HBB2 is an inducer of the KEAP1/NRF2/ARE pathway that reacts with sulfhydryl groups. Also, HBB2 upregulates Hsp70 in an HSF1-dependent manner. It appears that HBB2 reacts with cysteine residues of KEAP1, which leads to activation of NRF2, and binds to Hsp90 Cys that leads to activation of HST1.
H6039 1-(4-Hexyphenyl)-2-propane-1-one ≥98% (HPLC), oil Small molecular irreversible covalent inhibitor of thyroid hormone receptor-β (TRβ) interaction with coactivator (SRC2).
SML1260 HLM006474 ≥98% (HPLC) HLM006474 is a pan-E2F transcription factor inhibitor. E2F s part of the CDK/Rb/E2F pathway. When phosphorylated by CDKs, the tumor suppressor retinoblastoma protein (Rb) is inactivated, releasing E2Fs and allowing cell cycle progression. HLM006474 inhibited DNA-binding of all E2F complexes and down-regulated expression of E2F4 protein. HLM006474 induced apoptosis of A375 melanoma cells and synergized with paclitaxel in lung cancer cell lines.
SML0833 HLY78 ≥98% (HPLC) HLY78 is an activator of the Wnt/β-Catenin signaling pathway. HLY78 acts upstream of β-catenin synergistically with Wnt. It is believed to bind at a cavity at the dimeric interface of the Axin DIX domain, causing a conformational change of Axin to an active state, potentiating Axin–LRP6 association and promoting Wnt signaling transduction. There are several Wnt inhibitors used to study their potential in cancer therapy but few small molecules that activate the Wnt pathway. In Zebrafish, HLY78 increased the expression of the hematopoietic stem cell (HSC) transcription factors runx1 and cmyb, showing that it might be useful in HSC expansion, which could be important in transplantation and recovery after injury.
SML1696 HPB ≥98% (HPLC) HPB is a cell-permeable, non-cytotoxic N-hydroxybenzamide derivative that acts as a HDAC6-selective deacetylase inhibitor (IC50 = 31/376/677/842/1133 nM against HDAC6/8/10/1/7, >2 μM against HDAC2/3/4/11/9/5). HPB treatment results in reduced growth, but not viability (up to 64 μM and 72 hrs), of LNCaP prostate cancer cells and non-cancer human foreskin fibroblasts (IC50 = 8 and 16-32 μM, respectively), causing upregulated acetylation levels of alpha-tubulin and peroxiredoxin, but not histones, both in cultures and in mice in vivo. Intraperitoneal injection is efficacious in suppressing the expansion of prostate cancer CWR22 xenograft-derived tumors in mice (by 73% in 4 wks; Five daily 300 mg/kg i.p. dosings a week) without detectable weight loss.
SML0906 HPOB ≥98% (HPLC) HPOB is a very potent, selective inhibitor of HDAC6. HPOB inhibits proliferation of normal and transformed cell lines but does not induce cell death. The compound HPOB potentiates the effects of DNA-damaging cytotoxic anti-cancer drugs.
H1753 Hydralazine hydrochloride Inhibits DNA methyltransferase and modulates epigenetic regulation of gene expression. Non-selective MAO-A/B inhibitor; antihypertensive; semicarbazide-sensitive amine oxidase inhibitor.
SML0106 N-Hydroxy-4-(1-naphthalenyl)-benzamide ≥98% (HPLC) N-Hydroxy-4-(1-naphthalenyl)-benzamide is a cell-permeable, potent and selective HDAC8 inhibitor.
SML1158 (2S)-Hypusine dihydrochloride ≥95% (HPLC) (2S)-Hypusine is an unusual amino acid found only in eukaryotic translation initiation factor 5A (eIF5A) and a similar protein in archaebacteria. (2S)-Hypusine is formed by posttranslational modification of a lysine with the addition of the 4-aminobutyl moiety from the polyamine spermidine. There is increasing interest in the polyamine-hypusine axis and eIF5A, its a role in cell growth and differentiation, and a recent paper on the polyamine-hypusine axis as a potential new tumour suppressor network.
SML0551 Icaritin ≥98% (HPLC) Icaritin is a component of Epimedium flavonoid isolated from Herba Epimedii, which enhances osteoblastic differentiation of mesenchymal stem cells (MSCs) while it inhibits adipogenic differentiation of MSCs by inhibiting PPAR-g pathway. Icaritin has no effect on MSCs proliferation. Also, icaritin potently inhibits chronic myeloid leukemia (CML) and breast cancer cells proliferation most likely by modulation of MAPK/ERK/JNK and JAK2/STAT3 /AKT signaling. As other flavonoids, icaritin may exert estrogen-like activities.
SML0203 iCRT14 ≥98% (HPLC) iCRT14 belongs to the thiazolidinedione class of β-catenin-responsive transcription inhibitors. It decreases the levels of Dishevelled protein and modulates the binding of T-cell factor (TCF) to DNA. It results in consistent decrease in reduction of cell proliferation and tumor growth in colon cancer cells.
iCRT14 is a Wnt / β-catenin pathway inhibitor. It is a potent inhibitor of Catenin Responsive Transcription (CRT) reporter genes, as well as endogenous gene targets. iCRT14 also disrupts β-catenin-TCF4 interaction in a dose dependent manner, and causes G0/G1 arrest in colon tumor lines.
SML0211 iCRT3 The key mediator of Wnt signaling is the transcriptional co-activator b-catenin. In the cytoplasm, b-catenin is tightly bound to a complex that includes Axin and GSK-3b. Stimulation causes b-catenin stabilization, translocation to the nucleus and association with TCF4 to initiate transcription of responsive genes, referred to as Catenin Responsive Transcription (CRT). Virtually all Wnt-associated cancers are the result of misregulated CRT. Three inhibitors of CRT (iCRT) were identified in a screen that employed RNAi based knockdown of Axin, which stimulates CRT without affecting upstream mechanisms such as GSK activity, transduction by disheveled / frizzled, etc. These compounds are potent inhibitors of CRT reporter genes, as well as endogenous gene targets. The compounds also disrupt b-catenin-TCF4 interaction in a dose dependent manner, and cause G0/G1 arrest in colon tumor lines.
SML1898 Iguratimod ≥98% (HPLC) New Iguratimod (T-614) is an orally active anti-inflammatory compound that inhibits NF-kappaB (NF-KB) p65 subunit (RelA) phosphorylation and nuclear translocation (30 μg/mL against 10 ng/mL TNF-α; human synovial cells) without affecting IKBα degradation.
SML0969 Inauhzin ≥98% (HPLC) Inauhzin is a cell-permeable, selective inhibitor of SirT1, which effectively reactivates p53 by inhibiting SIRT1 activity. Inauhzin inhibits cell proliferation, induces senescence, and p53-dependent apoptosis of human cancer cells without apparent toxicity to normal cells.
SML0067 IOX1 ≥97% (HPLC) IOX1 (5-Carboxy-8-hydroxyquinoline) is a broad spectrum inhibitor of 2-oxoglutarate (2OG) oxygenases, including Jumonji C domain (JmjC) demethylases. It is useful for the study of histone demethylation and hypoxic sensing and results in translocation of active site iron on the 2OG oxygenases. For full characterization details, please visit the IOX1 probe summary on the Structural Genomics Consortium (SGC) website.

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SML0652 IOX2 ≥98% (HPLC) IOX2 is selective and potent inhibitor of prolyl hydroxylases (PHD). Stabilization of HIF-1R through inhibition of PHD has been examined as a potential treatment for ischemic diseases including anemia, myocardial infarction, and stroke. IOX2 is a selective inhibitor of the hypoxia inducible factor (HIF) prolyl-hydroxylases (PHD) that exhibits up-regulation of HIF1a in zebrafish. For full characterization details, please visit the IOX2 probe summary on the Structural Genomics Consortium (SGC) website.

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I4159 ITSA-1 ≥98% (HPLC), solid ITSA-1 is a suppressor of Trichostatin A (TSA) and a molecular tool for dissecting gene regulation by distinct aceytlation events (histone and tubulin). ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but not other HDAC inhibitors. ITSA-1 rreverses TSA induced histone acetylation, overall deacetylation. ITSA-1 also reverses TSA induced cell cycle arrest and apoptosis. Effective range 50 μM.
I0536 IWP-2 ≥98% (HPLC) IWP-2 is an inactivator of Porcn function; inhibitor of Wnt production. Wnt/b-catenin (‘canonical’) pathway maintains transcriptional programs that enable stem cells to remain multipotent. Hyperactivation of the Wnt/b-catenin pathway leads to disease stage. IWP-2 inhibits Wnt production. It appears that IWP inactivates Porcn function either by directly inhibiting the Porcn active site or by modulating the function of a Porcn regulator. Porcn is a member of the membrane-bound O-acyltransferase (MBOAT) family, which adds a palmitoyl group to Wnt proteins that is essential to their signaling ability and is required for Wnt secretion. IWP-2 is useful in both regenerative medicine and anticancer efforts.
SML0533 IWP-3 ≥98% (HPLC) IWP-3 is a Wnt inhibitor that prevents palmitylation of Wnt proteins by Porcupine (Porcn). IWP-3 is an inactivator of Porcn function that acts as inhibitors of Wnt production. Studies revealed that IWP-3 induces differentiation of human mesoderm cells to form cardiomyocytes.
SML1114 IWP-4 ≥95% (HPLC) IWP-4 is a potent inhbitor of the Wnt pathway regulatory protein porupine (Porcn). IWP-4 blocks palmitylation, and subsquent secretion and activity of Wnt. IWP-4 induces the differentiation of human pluripotent stem cells into cardiomyocytes.
SML0677 IWP12 ≥98% (HPLC) IWP12 is Wnt inhibitor that prevents palmitylation of Wnt proteins by Porcupine (Porcn), which is suitable for in vivo assays. IWP12 blocked post resection juvenile zebrafish tailfin regeneration.
J4829 JFD00244 ≥98% (HPLC), solid JFD00244 is a SIRT (sirtuin, human silent information regulator) inhibitor.
SML0808 JIB-04 ≥98% (HPLC) JIB-04 is a selective inihibitor of Jumonji demethylases without inhibiting other α-ketoglutarate-dependent hydroxylases or histone-modifying enzymes including amine oxidase LSD1 (also known as KDM1A), which demethylates histone lysines. JIB-04 is a pan-inhibitor of Jumonji demethylases with JARID1A (KDM5A) being the most sensitive (IC50=230 nM) followed by JMJD2D (IC50=290 nM) and JMJD3 (KDM6B) and JMJD2C (KDM4C) more resistant (IC50 855 and 1100 nM, respectively). JIB-04 selectively inhibited viability of several human cancer cell lines with little toxicity towards normal cells, and also diminished tumor growth in two separate xenograft mouse models.
J4455 JSH-23 ≥98% (HPLC), solid JSH-23 is an inhibitor of NF-kB nuclear translocation. It inhibits LPS and cytokine-induced nuclear translocation of the p65 subunit of NF-kB as analyzed by EMSA and western blot. The compound displays modest potency (IC50 7.1 uM in RAW 264.7), but has the unique property that it does not affect IkB degradation or recovery. The compound dose dependently inhibits LPS induced expression of cytokines, COX2 and iNOS, and presumably binds to, or interferes with the NLS of p65.
SML0630 JW55 ≥98% (HPLC) JW55 is a potent and selective inhibitor of Wnt/β-catenin signaling, that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2) leading to stabilization of AXIN2 followed by increased degradation of β-catenin. JW55 specifically inhibits canonical Wnt signaling that results in reduced cell-cycle progression, proliferation, and colony formation in colon carcinoma cell lines.
SML0324 JW67 ≥98% (HPLC) JW67 is an efficient and specific inhibitor of the canonical Wnt signaling in vitro and in vivo. It appears that JW67 affects the multiprotein complex consisting of β-catenin/GSK-3b/AXIN/APC/CK1 that controls the degradation of β-catenin. JW67 reduces growth of SW480 CRC cells in vitro by inhibiting cell-cycle progression at the G1/S phase.
SML0227 JW74 ≥98% (HPLC) JW74 is an efficient and specific inhibitor of the canonical Wnt signaling in vitro and in vivo. It appears that JW74 affects the multiprotein complex consisting of b-catenin/GSK-3b/AXIN/APC /CK1 that controls the degradation of b-catenin. JW74 reduces growth of SW480 CRC cells in vitro by inhibiting cell-cycle progression at the G1/S phase. JW74 also inhibits tumor formation and growth in the small intestine and colon of ApcMin mice.
SML0370 Kartogenin ≥98% (HPLC) Kartogenin induces the selective differentiation of multipotent mesenchymal stem cells (MSCs) into chondrocytes. Kartogenin binds to filamin A, and disrupts the specific interaction between filamin A and CBFβ (core-binding factor β subunit). Apparently, kartogenin induces chondrogenesis by regulating the nuclear localization of CBFβ.
SML1043 KC7F2 ≥98% (HPLC) KC7F2 is a cell permeable potent HIF-1 pathway inhibitor. KC7F2 inhibits the activation of HIF-target genes such as carbonic anhydrase IX, matrix metalloproteinase 2 (MMP2), enolase 1, and endothelin 1. KC7F2 suppresses the protein accumulation of HIF-1? in cancer cell lines by inhibition of its protein synthesis at the translation level. KC7F2 is preferentially cytotoxicity to cancer cells, an effect that is increased in hypoxia.
SML1588 KDOAM25 ≥97% (HPLC) KDOAM25 is a selective inihbitor of the KDM5 family histone demethylases JARID1A, JARID1B, JARID1C and JARID1D with IC50 values < 60 nM. JARID1A and JARID1B are independently overexpressed in some cancers with JARID1B (KDM5B, PLU1) also identified as a potential oncogene, a repressor of tumour repressor genes. JARID1C (KDM5C) and JARID1D (KDM5D) are located on the X- and Y-chromosomes respectively. KDOAM25′s closest off-target is JMJD2C (selectivity >400 fold). It shows no activity on other tested 2-OG family members, including FIH, NO66, MINA53 and PHD2. KDOAM25 is active in cells.
SML0619 KG-548 ≥97% (HPLC) KG-548 is an inhibitor of the hypoxia signaling transcription factor complex. Hypoxia inducible factor (HIF) is a heterodimer of two bHLH-PAS (basic Helix Loop Helix - Per-ARNT-Sim) subunits, including a HIF-α paralog (HIF-1α, -2α, -3α) and aryl hydrocarbon receptor nuclear translocator (ARNT, also known as HIF-β. KG-548 selectively binds within the ARNT PAS domain of the ARNT subunit of the HIF activator that recruits TACC3 (Transforming Acidic Coiled Coil Containing Protein 3) coactivator, competing with TACC3 for binding to the ARNT PAS-B domain and thus acting as as an ARNT/TACC3 disruptor.
SML1866 KIN1408 ≥98% (HPLC) New KIN1408 is a small molecule that targets factors at or above the level of MAVS in the RLR signaling pathway to drive IRF3 activation (IRF3 nuclear translocation ECmax = 5 μM in 20 h; Huh7 cells) without significant cytotoxicity (50 μM/20 h in Huh7 or 20 μM/36 h in HEK293 cultures). KIN1408 induces cellular transcription of innate immune genes (Eff. conc. 1.25-20 μM in 20 h; PMA-differentiated THP-1 cells) in a MAVS- and IRF3-dependent manner and exhibits broad-spectrum anti-viral activity (Eff. conc. 1-5 μM), including dengue virus 2 (DV2; Huh7), influenza A (IAV H3N2; HEK293), RSV (A2 strain; HeLa), Ebola (EBOV strain Zaire; HUVECs), Nipah virus (NiV; HUVECs), and Lassa virus (LASV; HUVECs). MAVS signaling activation upon Zika virus infection or KIN1408 treatment is reported to result in pTBK1 mitochondria relocalization and caspase 3-mediated apoptosis in human neuroepithelial stem (NES) cells.
SML1032 KL001 ≥98% (HPLC) KL001 stabilizes cryptochrome (CRY), preventing ubiquitin-dependent degradation. CRY proteins are part of a feedback loop, acting as transcription repressors to inhibit CLOCK-BMAL1 components of the circadian clock. KL001 stabilization of CRY proteins results in lengthening of the circadian period, and also inhibited glucagon-induced gluconeogenesis in primary hepatocytes. Other compounds affecting circadian rhythms include Casein kinase I (CKI) inhibitors such as longdaysin (Sigma Prod. No. SML0127) and synthetic ligands for the nuclear receptors REV-ERB such as SR8278 (Sigma Prod. No. S9576), but KL001 appears to be the first small molecule that specifically acts on CRY proteins.
SRP3101 KLF4-TAT human recombinant, expressed in HEK 293 cells, ≥90% (SDS-PAGE), ≥90% (HPLC), cell culture tested KLF4 is a member of the Kruppel-like factor (KLF) family of zinc finger transcription factors. Recombinant human KLF4-TAT is a 51.7 kDa protein containing 483 amino acid residues, including 13- residue C-terminal TAT peptide.
SML0948 KY02111 ≥98% (HPLC) KY02111 promotes differentiation of human pluripotent stem cells (hPSCs) to cardiomyocytes by inhibiting WNT signaling in hPSCs in a manner that is distinct from that of previously studied WNT inhibitors. The substantial (98%) differentiation of hPSCs to cardiomyocytes with KY02111 is achieved in xeno-free and cytokine-free conditions.
SML1831 KYA1797K potassium salt ≥98% (HPLC) KYA1797K is an inhibitor of both Wnt/β-catenin and Ras pathways. It binds to the axin regulators of the G-protein signaling (RGS) domain enhancing formation of the β-catenin destruction complex and inducing activation GSK3β, which results in phosphorylation and subsequent degradation of both β-catenin and K-Ras. KYA1797K was show to suppress tumor growth and progression in mouse xenografts of CRC cells that had APC and K-Ras mutations.
SML0759 L002 ≥98% (HPLC) L002 (NSC764414) is an inhibitor of acetyltransferase p300, a lysine acetyltransferase that catalyzes acetyl group attachment to lysine residues of a variety of proteins including histones and p53, and acts as a critical coactivator of several oncogenic transcription factors involved in cancer cell survival and proliferation including STAT3, NF-kB, and hypoxia-inducible factor-1α (HIF-1α). L002 (NSC764414) was discovered from compounds assayed for cytotoxicity to the triple-negative breast cancer (TNBC) cell line MDA-MB-231 but not to the human mammary epithelial cells, then further screened for inhibition of p300. L002 has an in vitro IC50 of 1.98 μM for p300 with lesser inhibition of the GNAT (GCN5-related N-acetyltransferase) family, and no inhibition against the MYST family of histone acetyltransferases (HATs), histone deacetylases (HDACs), or histone methyltransferases (HMTs). L002 potently suppressed tumor growth and histone acetylation of MDA-MB-468 xenografts and leukemia and lymphoma cell lines.
SML1752 LF3 ≥98% (HPLC) LF3 is a potent inhibitor of Wnt/β-catenin signaling that suppresses cancer cells motility, cell-cycle progression, and the overexpression of Wnt target genes. LF3 is a potent and specific antagonist of the interaction between β-catenin and the transcription factor TCF4. LF3 blocks self-renewal of cancer stem cells.
SML1279 LLY-507 ≥97% (HPLC) LLY-507 is a potent and selective inhibitor of SMYD2 protein lysine methyltransferase (PKMT) with an in vitro IC50 <15 nM and >100-fold selectivity over other methyltransferases and other non-epigenetic targets. LY-507 has been shown to inhibit p53K370 monomethylation in cells with an IC50 ~600 nM. For full characterization details, please visit the LLY-507 probe summary on the Structural Genomics Consortium (SGC) website.

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SML1053 LMK235 ≥98% (HPLC) LMK235 is a histone deacetylase (HDAC) inhibitor with greater potency against HDAC4 and HDAC5 (IC50 = 11.9 and 4.2 nM, respectively) than other HDAC family members (IC50 values = HDAC1 320 nM, HDAC2 881 nM, HDAC6 55.7 nM, and HDAC8 1278 nM). LMK235 potentiates the cytotoxic effects of cisplatin, and sensitizes platinum-drug resistant tumor cell lines to cisplatin toxicity.
SML1628 LMT-28 ≥98% (HPLC) LMT-28 is an IL-6 antagonist that targets the IL-6 Receptor β subunit, Glycoprotein 130 (gp130). Its binding to gp130) results in inhibition of IL-6 activation, and downregulation of levels of p-STAT3. LMT-28 was shown to stimulate phosphorylation of STAT3 and JAK2 protein. IL-6 dysregulation is involved in inflammation and cancers. LMT-28 had inhbitory activity against IL-6–dependent TF-1 cell proliferation and also had therapeutic effect against pancreatitis.
SML1499 LW479 ≥98% (HPLC) LW479 is a potent histone deacetylase inhibitor (HDACI) that down-regulates EGFR expression. Apparently, LW479 blocks the binding of the transcription factor Sp1 and HDAC1 to the EGFR promoter region. LW479 potently induces cell cycle arrest and apoptosis breast cancer cell lines. Also LW479 suppressed breast tumor growth and pulmonary metastasis in nude mice.
M5820 M344 ≥98% (HPLC), powder M344 is a HDAC inhibitor; subtype selective for HDAC6 over HDAC1. M344 inhibits HDAC (IC50 = 100 nM) and also inhibits hyperacetylation of histone H4, terminal cell differentiation, transcription (γ-globin), and tumor cell death.
M1824 MC1568 ≥97% (HPLC) MC1568 is a selective class II (IIa) histone deacetylas (HDAC II) inhibitor.
M4949 2’-C-Methylcytidine ≥95% (HPLC), powder 2′-C-Methylcytidine is a potent inhibitor of the HCV NS5B RNA polymerase. 2′-C-Methylcytidine was the first nucleoside NS5B inhibitor that showed clinical efficacy. 2′-C-Methylcytidine was found to be effective against the 17D vaccine strain of yellow fever virus YFV in cell culture.
SML0713 2′-C-Methylguanosine ≥98% (HPLC) 2′-C-Methylguanosine (2’-MeG) is a potent and specific RNA dependent RNA polymerase NS5B inhibitor of the hepatitis C virus (HCV).
SML0343 Methylstat ≥98% (HPLC) Methylstat is an inhibitor of the Jumonji C domain-containing histone trimethyl demethylases (JHDMs). Methylstat inhibits the activity of JMJD2C (IC50 = 4.3 μM), with similar potency against JMJD2E and JMJD3. The compound has poor activity against dimethyl demethylases, and does not inhibit class I or II HDACs. Methylsat blocks proliferation of the esophageal carcinoma cell line KYSE150 with an IC50 value of 5.1 μM.
SML0537 MI-1 ≥98% (HPLC) MI-1 is a Menin-MLL interaction inhibitor. The mixed lineage leukemia (MLL) gene encodes MLL, a histone methyltransferase important in regulating gene transcription. MLL rearrangements and formation of fusion oncoproteins can block hematopoietic differentiation and increase proliferation, resulting in acute leukemias. Menin, encoded by the MEN1 gene, is a tumor suppressor associated with multiple endocrine neoplasia type 1. It also acts as an oncogenic co-factor of MLL fusion proteins. MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 micromolar.
SML1451 MI192 hydrochloride ≥98% (HPLC) MI192 is a potent and selective histone deacetylase 3 (HDAc 3) inhibitor that inhibits IL-6 production in peripheral blood mononuclear cells (PBMCs) from rheumatoid arthritis (RA) but not healthy PBMCs.
SML1585 ML116 ≥95% (HPLC) ML116 is a potent and selective inhibitor of STAT3 (signal transducer and activator of transcription 3) phosphorylation. ML116 potently inhibits growth and induces cell death of rodent and human glioma cells. ML116 is inactive against the related STAT1 and NFkB anti-targets.
STAT3 is a transcription factor which is activated by cytokines and growth factors. It is oncogenic and is present in various cancers, such as breast, prostate, renal cell, melanoma, ovarian, lung, leukemia, lymphoma and myelomas. It is associated with cellular growth, survival and malignancy.
SML0290 MLS000389544 ≥98% (HPLC) MLS000389544 is a selective and potent methylsulfonylnitrobenzoate thyroid hormone receptor β (TRβ) antagonist that blocks the association of TRβ with steroid receptor coactivator 2 (SRC2). It effectively block TR-mediated gene transcription. MLS000389544 is selective for TR over other NR family members. It appears to act by irreversible mechanisms and target cysteine residues in the coactivator binding pocket.
SML1673 MM-206 ≥98% (HPLC) MM-206 is a cell-permeable, non-cytotoxic naphthalene sulfonamide compound effectively inhibits STAT3 DNA-binding activity (IC50 = 2.45 μM). MM-206 inhibits G-CSF-stimulated STAT3 phosphorylation in human AML cells (IC50 = 0.8-1.9 μM) and exhibits higher apoptosis-inducing potency in AML (EC50 in μM = 6.3/p198, 7.1/MV4-11 and 7.6/HL-60) than ALL cultures (EC50 in μM = 26.0/KOPN-8 & 42.2/RS4-11). When administered via daily i.p. dosing (30 mg/kg), MM-206 is efficacious in prolonging the survival of mice received MV4-11 AML xenograft.
SML1012 MN-64 ≥98% (HPLC) MN-64 is a very potent inhibitor of Tankyrase 1 and 2 (IC50 = 6 and 72 nM, respectively). The compound MN-64 blocks Wnt signaling in HEK293 cells containing a Wnt pathway reporter system.
M2195 MOCPAC ≥95% (HPLC), solid Selective HDAC1 substrate (over HDAC6, class I over class II).
SML1555 MS023 hydrochloride ≥98% (HPLC) MS023 is a potent and selective chemical probe for Type I protein arginine methyltransferases (PRMTs). MS023 is a potent inihbitor of PRMTs 1,3,4,6,and 8 (IC50 = 30, 119, 83, 8, and 8 nM, respectively), which are responsible for asymmetric dimethylation of arginine residues. MS023 is active in cells. For full characterization details, please visit the MS023 probe summary on the Structural Genomics Consortium (SGC) website.

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SML1553 MS049 hydrochloride ≥98% (HPLC) MS049 is a potent and selective inhibitor of protein arginine methyltransferases (PRMTs) PRMT 4 and PRMT6. MS049 is active in cells. For full characterization details, please visit the MS049 probe summary on the Structural Genomics Consortium (SGC) website.

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SML1405 MS37452 ≥98% (HPLC) MS37452 is a selective Chromobox homolog 7 (CBX7) modulator that disrupts CBX7ChD binding to H3K27me3. MS37452 inhibits CBX7 binding to INK4/ARF gene locus, and induces decline of p14/ARF and p16/INK4a in human PC3 cells.
SML1726 MSAB ≥95% (HPLC) A cell-permeable compound that targets β-catenin via direct affinity interaction within the C-terminal two thirds (a.a. 301-670) of the Armadillo repeat region (a.a. 136–686), inducing β-catenin ubiquitination and proteasomal degradation (Eff. conc. 1.25-5 μM in DLD-1, SW480 and LS174T cultures). MSAB selectively inhibits against Wnt sginaling-dependent proliferation of cancer cells (IC50 <6 μM), while exhibiting little efficacy in Wnt-independent cultures (<10% inhibition at 10 μM). Likewise, daily intraperitoneal injection (10-20 mg/kg/day) is efficacious in suppressing the expansion of established tumors from HCT116, HT115, and H23 xenografts in mice, while exhibiting little efficacy against the Wnt-independent H460 tumor growth.
N3289 N2-Ethyl-2′-deoxyguanosine ≥98% (HPLC), solid  
SRP3119 NANOG human recombinant, expressed in E. coli, ≥98% (SDS-PAGE), ≥98% (HPLC), cell culture tested NANOG is one of the central genes regulating self-renewal and pluripotency capacities of embryonic stem cells (ESC). Constitutive expression of this gene prevents the differentiation of ESCs, and along with SOX2 (SRY-box 4) and OCT-4 (octamer-binding transcription factor 4), it regulates pluripotency-related gene expression and maintains the pluripotency of ESCs. During ESC differentiation both these genes are down-regulated, and gene profiling shows that the expression of NANOG is uniformly high in ESC lines. There is significant similarity between ESC and carcinoma in situ testis (CIS), including the high expression of NANOG. It is novel marker for testicular CIS and germ cell tumors. NANOG shows abnormal expression in a variety of human cancers, such as carcinomas of the brain, oral cavity, head and neck, breast, lung, liver, pancreas, kidney, gastric, cervix, ovary, prostate, and colon. This expression is also related to treatment resistance and poor survival of cancer patients.
SRP3120 NANOG TAT human recombinant, expressed in E. coli, ≥95% (SDS-PAGE), ≥95% (HPLC), cell culture tested Nanog is a regulatory protein that is associated with undifferentiated pluripotent cells. Recombinant human Nanog-TAT is a 36.2 kDa protein, which is synthesized as a 304 amino acid polypeptide plus a 13- residue C-terminal TAT peptide.
SML0078 1-Naphthohydroxamic Acid ≥98% (HPLC) 1-Naphthohydroxamic Acid is a cell-permeable, potent, and selective histone deacetylase 8 (HDAC8) inhibitor. 1-Naphthohydroxamic acid selectively inhibits HDAC8 (IC50 = 14 μM) over class I HDAC1 and class II HDAC6 (IC50 >100 μM). Treatment of cells with 1-Naphthohydroxamic acid does not increase neither global histone H4 nor tubulin acetylation . Also in contrast to the pan-HDAC inhibitors the compound is not reducing total intracellular HDAC activity.
SML1538 NMDI14 ≥97% (HPLC) NMDI14 is a potent nonsense-mediated RNA decay (NMD) inhibitor. NMDI14 targets a pocket in the SMG7 protein and disrupts SMG7–UPF1 interactions. NMDI14 restores of full-length p53 protein activity in in cells with premature termination codons (PTC) mutated p53.
SML0267 NSC 162535 disodium salt ≥98% (HPLC) NSC 162535 is an inhibitor of RNA editing in trypanosomatid pathogens that results from lost of the interaction of core editosome with substrate RNA.
SML1428 O4I2 ≥98% (HPLC) O4I2 is a potent inducer of the Octamer-binding transcription factor 4 (Oct3/4) in various human cell lines including human fibroblasts. In principle O4I2 could be a useful tool for chemical-mediated induction of pluripotency in somatic cells.
SML0651 OAC1 ≥98% (HPLC) OAC1 enhances iPSC reprogramming efficiency by enhancing Oct4 and Nanog driven gene expression. Treatment of mouse embryonic fibroblasts transduced with Oct2, Sox2, Klf4 and c-myc displayed a two-fold increase in the formation of ESC-like clones. OAC1 treated cells display a hypomethylated state of Oct4 promoter DNA.
SML1650 OAC2 ≥97% (HPLC) OAC2 (Oct4 activating compound 2) is an activator of Octamer-binding transcription factor 4 (Oct4), which is involved in the self-renewal of undifferentiated embryonic stem cells, regulating embryonic stem cell pluripotency.
SML1383 OG-L002 hydrochloride ≥98% (HPLC) OG-L002 is a recently developed inhibitor with IC50 of 20 nM at LSD1 and much lower activity at MAO-A and MAO-B (1.38 and 0.72 μM, respectively). OG-L002 exhibits potent anti-viral activity in vitro and in mouse models of HSV infection. Lysine specific demethylase 1 (LSD1) is a histone demethylase that removes methyl groups from lysine 4 or 9 of H3 histone tails. Inhibition of LSD1 leds to suppression of herpes simplex and herpes zoster viral infections and viral reactivation from latency. MAO inhibitors (pargyline, tranylcypromine) are known to inhibit LSD1, but with low potency and selectivity. OG-L002 is a more selective and potent tool for LSD1 inhibition.
SML1209 OICR-9429 ≥98% (HPLC) OICR-9429 is a cell penetrant, potent and selective antagonist of the interaction of WDR5 (WD repeat domain 5) with peptide regions of MLL and Histone 3 that potently binds to WDR5. OICR-9429 inhibits the interaction of WDR5 with MLL1 and RbBP5 in cells. For full characterization details, please see OICR-9429 on the Structural Genomics Consortium (SGC) website.

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O9390 N-Oxalylglycine ≥98% (HPLC) N-Oxalylglycine is an inhibitor of α-ketoglutarate-dependent enzymes and mimics the initial steps but does not initiate the hydroxylation process. N-Oxalylglycine has been used to inhibit Jumonji C-domain-containing histone lysine demethylases.
SRP2079 p300 human recombinant, expressed in insect cells, ≥70% (SDS-PAGE) Human p300 and CBP (CREB binding protein) are highly related transcriptional coactivators. Both proteins have been identified through protein interaction assays. In addition to interacting with a variety of cellular factors and onco-proteins, loss of the wild type CBP alleles in isolated tumors suggests that CBP/p300 might serve as tumor suppressors. The ability of p300 to acetylate many transcription factors, including p53, E2F, TFIIE, and TFIIF etc. demonstrates a novel mechanism of targeted p300 regulation of gene expression.
SRP2086 p300 (C1135-2414) human recombinant, expressed in insect cells, ≥70% (SDS-PAGE) Human p300 and CBP (CREB binding protein) are highly related transcriptional coactivators. Both proteins have been identified through protein interaction assays. In addition to interacting with a variety of cellular factors and onco-proteins, loss of the wild type CBP alleles in isolated tumors suggests that CBP/p300 might serve as a tumor suppressor. The C-terminus of p300 contains a histone acetyltransferase (HAT) domain expanded from residues 1195 to 1673, an activation domain (residues 1763-1812) that interacts with many transcription factors and an SRC-1 domain further down stream of the activation domain. P300 is able to acetylate histones and many other transcription factors, including p53, E2F, TFIIE, and TFIIF etc. implicating diverse roles of p300 in gene regulation.
SRP2096 p300-Ch1 (302-531) human recombinant, expressed in E. coli, ≥80% (SDS-PAGE) Human p300 and CBP (CREB binding protein) are highly related transcriptional coactivators. Both proteins have been identified through protein interaction assays. In addition to interacting with variety of cellular factors and onco-proteins, loss of the wild type CBP alleles in isolated tumors suggests that CBP/p300 might serve as tumor suppressors. The ability of p300 to acetylate many transcription factors, including p53, E2F, TFIIE, and TFIIF etc. demonstrated a novel mechanism of targeted p300 regulation of gene expression.
SML1058 PBIT ≥98% (HPLC) PBIT is a potent inhibitor of JARID1B (KDM5B) histone lysine demethylase that inhibits removal of H3K4me3 in UACC-812 cells. PBIT inhibits proliferation of cells overexpressing JARID1B. PBIT is selective for JARID1 enzymes and does not inhibit demethylases UTX or JMJD3.
M0688 Pedibin precursor peptide >92% (HPLC), solid  
SML0667 PF-429242 dihydrochloride ≥98% (HPLC) PF-429242 is a potent inhibitor of S1P (cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease) that reduces expression levels of hepatic SREBP target genes and lower rates of cholesterol and fatty acid synthesis in mice. PF-429242 is a potent antiviral agent against prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV in cultured cells. PF-429242 efficiently prevented the processing of GPC from the LCMV and LASV. PF-429242 is expected to be active against CCHFV.
SML1408 (R)-PFI-2 ≥97% (HPLC) (R)-PFI-2 is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (also known as SET9). (R)-PFI-2 has an IC50 value of 2 nM and 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. For full characterization details, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.

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PZ0312 (S)-PFI-2 (S)-PFI-2 is the negative control probe for (R)-PFI-2 hydrochloride (catalog no. SML1408), which is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (SET9). (R)-PFI-2 has 1000-fold selectivity for SETD7 (SET9) over other methyltransferases and other non-epigenetic targets and an IC50 value of 2 nM. (S)-PFI-2 is 500-fold less active. For characterization details of (R)-PFI-2 and (S)-PFI-2, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.

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SML0026 4-Phenylbutyryl hydroxamic acid ≥98% (HPLC) 4-Phenylbutyryl hydroxamic acid is a cell permeable HDAC inhibitor which is about 100 times more potent than parent carboxylic acid among nine HDAC enzymes.
SML0920 α-Phenyl tropolone ≥98% (HPLC) α-Phenyl tropolone is a very potent inhibitor of the hisotne deacetylases HDAC2 and HDAC8 (Ki = 0.26 and 1.09 nM, respectively). The compound, α-Phenyl tropolone, does not affect other HDAC isoforms up to concentrations of 20 μM, with the exception of HDAC 6 (Ki = 527 nM).
SML0313 Pimelic Diphenylamide 106 ≥98% (HPLC) 106 is a Class I HDAC inhibitor, demonstrating no activity against class II HDACs. It is a slow, tight-binding inhibitor of HDACs 1, 2, and 3, with a preference toward HDAC3 with Ki of 14 nM, 15 times lower than the Ki for HDAC1.
P0083 PRMT1 from rat recombinant, expressed in E. coli, ≥90% (SDS-PAGE), buffered aqueous solution Methyl transferases catalyze the addition of methyl groups to nitrogen, carbon, sulfur, and oxygen atoms of small molecules, lipids, proteins, and nucleic acids. Eight mammalian protein arginine methyltransferases (PRMT) have been identified. PRMT1 is the predominant member of the methyl transferases, which catalyzes the protein arginine N-methylation reactions. PRMT1 is implicated in various cellular processes including: transcription, RNA processing, and signal transduction.
P9391 Procainamide hydrochloride Inhibits DNA methyltransferase and modulates epigenetic regulation of gene expression. Na+ channel blocker and Class IA anti-arrhythmic.
P5874 PTACH ≥98% (HPLC), solid HDAC inhibitor; more potent than the majority of HDAC inhibitors except for SAHA (gold standard).
SML0296 Pyroxamide ≥97% (HPLC) Pyroxamide is an inhibitor of HDAC1 (IC50 = 100 nM). Pyroxamide induces apoptosis and cell cycle arrest in leukemia, bladder and prostate cancer cell lines.
SML1865 Rbin-2 ≥98% (HPLC) Rbin-2 (ribozinoindole-2) is a cell penetrant, potent, selective and reversible inhibitor of Midasin that inhibits eukaryotic ribosome biogenesis. Rbin-2 directly targets AAA+ ATPase Midasin.
SML1112 Remodelin hydrobromide ≥98% (HPLC) Remodelin is an inhibitor of acetyl-transferase NAT10, a nucleolar N-acetyltransferase involved in stabilization of microtubules. Remodelin was found to correct cell defects associated with progeria, improving nuclear shape and reducing the DNA damage believed to be associated with mutations in the gene for laminin A. Although the mechanism is still being studied, microtubule stability appears to be involved. Remodelin inhibition of NAT10 activity in laminopathic cells appears to result in reduced microtubule anchorage, normalizing the nuclear shape of laminopathic cells. Remodelin should be a useful tool to study how NAT10 affects nuclear architecture and its relationship to and possible treatments for laminopathies and aging and as well as its over-expression found in a variety of soft tissue sarcomas.
R8279 RG108 ≥98% (HPLC), powder RG108 is a DNA methyltransferase (DMNT) inhibitor. It reactivates tumor suppressor gene expression (p16, SFRP1, secreted frizzled related protein-1, and TIMP-3) in tumor cells by DNA demethylation. RG108 also inhibits human tumor cell line (HCT116, NALM-6) proliferation and increased doubling time in culture.
SML1652 RGFP966 ≥98% (HPLC) RGFP966 is a selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 value of 80 nM and no inhibition of any other HDACs at concentrations up to 15 μM. In mouse studies, RGFP966 facilitated extinction of cocaine-seeking behavior and enhanced long-term object memory acquisition and consolidation. In a rat study, RGFP966 ameliorated amyloid-β oligomer-induced synaptic plasticity impairment. RGFP966 was also found to reduce proliferation and inducd differentiation in mouse lymphoid and myeloid malignancies.
R3501 Rifampicin ≥97% (HPLC), powder Inhibits the assembly of DNA and protein into mature virus particles.
Mode of Action: Inhibits initiation of RNA synthesis by binding to β-subunit of RNA polymerase.
Rifampicin inhibits the assembly of DNA and protein into mature virus particles. It inhibits initiation of RNA synthesis by binding to β-subunit of RNA polymerase, which results in cell death.
R7382 Rifampicin plant cell culture tested, BioReagent, ≥97% (HPLC), crystalline Inhibits the assembly of DNA and protein into mature virus particles.
Mode of Action: Inhibits initiation of RNA synthesis by binding to β-subunit of RNA polymerase.
R9407 RM-65 ≥98% (HPLC) RM-65 is an arginine methyltransferase inhibitor and is cell (HepG2) permeable.
SML1175 Romidepsin ≥98% (HPLC) Romidepsin is a very potent natural prodrug inhibitor of HDAC1 and HDAC2 that is converted to active form by glutathione. Romidepsin has IC50 values of 36 nM and 47 nM for HDAC1 and HDAC2, respectively. Romidepsin kills lymphoma cell lines overexpressing Bcl-2 and Bcl-XL, and has been approved for the treatment for cutaneous T-cell lymphoma (CTCL) and peripheral T-cell lymphoma, and a variety of other cancers.
SML1113 RSC133 ≥98% (HPLC) RSC133 is an epigenetic modulator that effectively enhances reprogramming of human somatic cells and maintenance of human stem cell pluripotency. Apparently, RSC133 facilitates the reprograming by dual inhibition of histone deacetylase and DNA methyltransferase activities. In hFFs, RSC133 rapidly activates pluripotency-associated genes Nanog, Oct4, and Rex1 up to 2- to 2.5-fold. RSC133 exerts positive effects on cell proliferation and ablates pro-senescence phenotypes.
R1408 RU7 ≥98% (HPLC) RU7 is a selective inhibitor of bacterial β-clamp interaction with DNA polymerase POL III, and an inhibitor of a DNA polymerase sliding clamp. Sliding clamps are proteins which function with diverse DNA polymerases, repair factors, and cell cycle-control proteins. RU7 binds to the peptide-binding pocket of the β-clamp and selectively inhibits Pol III, compared with Pol II and Pol IV.
SML0330 S3I-201 ≥97% (HPLC) S3I-201 is a cell-permeable Stat3 inhibitor that binds to the Stat3-SH2 domain, prevents Stat3 phosphorylation/activation, dimerization, and DNA-binding.
SML0061 SAHA ≥98% (HPLC) SAHA or Vorinostat facilitates the transcription of genes that result in apoptosis, differentiation and growth arrest. It has been observed to give beneficial results in lymphoma but not in solid tumors.
Vorinostat or suberoylanilide hydroxamic acid (SAHA) is a potent, reversible pan-histone deacetylase (HDAC) inhibitor. It inhibits both class I and class II HDACs, altering gene transcription and inducing cell cycle arrest and/or apoptosis in a wide variety of transformed cells.
S8825 Salermide ≥98% (HPLC) Salermide is a novel Sirtuin 1 (Sirt1) and Sirtuin 2 (Sirt2) inhibitor (III histone deacetylases inhibitor). In vitro Salermide has a stronger inhibitory effect on Sirt2 than on Sirt1. Salermide induces massive apoptosis in tumor cells. The activity was ascribed to effect of Salermide to the reactivation of proapoptotic genes epigenetically repressed exclusively in cancer cells by Sirt1. Salermide is a stronger Sirtuin inhibitor than sirtinol (Cat. No.S7942).
SML1054 SBI-0087702 ≥98% (HPLC) SBI-0087702 promotes the cytoplasmic localization of ATF2 in melanoma cells. SBI-0087702-induced translocation of ATF2 to the mitochondria results in increased apoptosis due to loss of mitochondrial membrane integrity. SBI-0087702 also inhibits growth and motility of melanoma cells. SBI-0087702 was shown to inhibit ATF2 phosphorylation on Thr52 by PKCε.
SML0763 SC144 hydrochloride ≥98% (HPLC) SC144 is a potent inhibitor of glycoprotein 130 (gp130). SC144 binds to gp130 and blocks STAT3 phosphorylation, nuclear translocation and expression of STAT3 responsive genes. SC144 inhibits the growth of several tumor cell lines, independent of p53 or hormone receptor levels, and inhibits growth of ovarain tumor xenografts in mice.
S7817 Scriptaid ≥95%, solid Histone deacetylase inhibitor with lower toxicity than trichostatin A; used to enhance protein expression.
Scriptaid inhibits the cell cycle progression of ovarian cancer cells by inducing arrest in G0/G1 and/or G2/M phase. Treatment of cells with scriptaid results in loss of mitochondrial membrane potential and increased acetylation of H3 and H4 histone tails.2 Sciptaid induces expression of γ-globin in human erythroid progenitors via p38 signaling and may be a treatment option for sickle cell disease.3 It enhances the transcriptional activity and protein expression in mouse embryos. This is useful in producing cloned, inbred mouse embryos that develop normally into adulthood with regular reproductive ability.4
SML1107 SGC0946 ≥98% (HPLC) SGC0946 is a potent and selective inhibitor of Histone H3-lysine79 (H3K79) methyltransferase DOT1L with an IC50 of 0.3 nM in a radioactive enzyme assay, and over 100-fold selectivity for DOT1L over other histone methyltransferases. In cell studies, SGC0946 reduces H3K79 dimethylation with an IC50 of 2.6 nM in A431 cells and 8.8 nM in MCF10A cells. SGC0946 was found to selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia. For full characterization details, please visit the SGC0946 probe summary on the Structural Genomics Consortium (SGC) website.

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SML1242 SGC707 ≥98% (HPLC) SGC707 is a potent allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). SGC707 has an IC50 value of 50 nM and >100-fold selectivity over other methyltransferases and non-epigenetic targets. SGC707 binds to PRMT3 with KD of 50 nM (ITC), and inhibits histone methylation in cells with an IC50 value below 1 μM. For full characterization details, please visit the SGC707 probe summary on the Structural Genomics Consortium (SGC) website.

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SML1358 SGI-1027 ≥98% (HPLC) SGI-1027 is a DNA methyltransferase (DNMT) inhibitor with IC50 values of 6-13 μM for DNMT3B, DNMT3A and DNMT1. SGI-1027 directly inhibits DNMT activity by competing with the cofactor, S-adenosylmethionine (SAM) in the methylation reaction. SGI-1027 treatment of cancer cell lines induced degradation of DNMT1, but not DNMT3A or DNMT3B, and in RKO cells caused re-expression of the silenced tumor supressor genes p16, MLH1 and TIMP3.
SML1514 SirReal2 ≥98% (HPLC) SirReal2 is a potent and selective inhibitor of Sirt2, an NAD-dependent lysine deacetylase that has been implicated in the pathogenesis of cancer, inflammation, and neurodegeneration. SirReal2 has an IC50 value of 140 nM and is >1000-fold selective for Sirt2 over Sirt1 and Sirt3. SirReal2 is believed to act through a ligand-induced structural rearrangement of the active site, binding at an adjacent pocket to lock Sirt2 in an open conformation. SirReal2 caused to tubulin hyperacetylation in HeLa cells and destabilization of the checkpoint protein BubR1, consistent with Sirt2 inhibition.
S8446 SIRT1 human recombinant, expressed in E. coli, N-terminal histidine tagged, ≥90% (SDS-PAGE), buffered aqueous glycerol solution Sirtuins are a family of NAD+ dependent deacetylases that remove an acetyl group from the e-amino group of lysine residues. The proteins within this family are named after the first protein discovered, from yeast, called Sir2 (Silent Information Regulator 2). The proteins are conserved from bacteria to higher eukaryotes. In humans, there are seven Sir2 family members (SIRT1 to SITR7). SIRT1 plays a pivotal role in the regulation of cellular differentiation, metabolism, cell cycle, apoptosis and regulation of p53. Several targets for SIRT1 were identified among them Lys382 of p53. Using RNA interference, additional targets were identified. It was demonstrated that reduced levels of human SIRT1 led to increased acetylation of Histone H4-Lys16, H4-Lys20, and Histone H3-Lys9 as well as histone H1-Lys26.
CS1040 SIRT1 Assay Kit sufficient for 100 assays Sirtuins (Sir2) are an evolutionarily conserved family of NAD+ dependent histone/protein deacetylases that tightly couple the cleavage of NAD+ and the deacetylation of protein substrates. The reaction products are nicotinamide, the deacetylated product, and a novel metabolite, 2′-O-acetyl-ADP-ribose. The proteins within this family are named after the first protein discovered from this family, Sir2 (Silent Information Regulator 2). Besides gene silencing, sirtuin proteins are important in other processes such as cell cycling regulation and fatty acid metabolism. SIRT1 is the human homolog of Sir2 and the one most studied to date. SIRT1 mediates p53 dependent process, transcription regulation, muscle differentiation, adipogenesis, and protection from axonal degeneration. SIRT1 also participates in early embryogenesis, neurogenesis, and cardiogenesis.
S7942 Sirtinol ≥95% (NMR) Sirtinol inhibits yeast Sir2p transcriptional silencing activity in vivo, yeast Sir2p and human SIRT2 deacetylase activity in vitro. It inhibits the physiological regulators of platelet aggregation such as thrombin and collagen, attenuates intracellular Ca2+ release and formation thromboxane B2. It may increase levels of cAMP by inhibition of cAMP phosphodiesterase and inhibit the aggregation of platelets.2 Sirtinol reduces inflammatory responses of human dermal microvascular endothelial cells to TNF-α and IL-1β.3
Sirtinol inhibits yeast Sir2p transcriptional silencing activity in vivo, yeast Sir2p, and human SIRT2 deacetylase activity in vitro.
SML0454 SM-7368 ≥98% (HPLC) SM-7368 is a cell-permeable inhibitor of TNF-α-induced MMP-9 upregulation. Also, SM-7368 strongly inhibits TNF-α-induced NF-kB activity but not AP-1 activity. The compound inhibits the TNF-α-induced invasion of HT1080 human fibrosarcoma cell line.
SML0309 Sodium phenylbutyrate ≥98% (HPLC) Sodium phenylbutyrate is a histone deacetylase inhibitor.
S4068 Splitomicin ≥98% (HPLC), powder Sir2p (silent information regulator) and HDAC inhibitor.
Splitomicin, a derivative of β-naphthol is an inhibitor of Silent Information Regulator 2 (SIR2). It inhibits the NAD+-dependent deacetylase activity of Sir2 in vitro. It increases the levels of cyclic AMP by inhibiting the activity of cyclic AMP phosphodiesterase, interferes with mobilization of intracellular Ca+2 and ATP release. This results in inhibition of platelet aggregation that is effective in cardiovascular and cerebrovascular diseases.
SML0154 SPV-106 ≥98% (HPLC) SPV106 is a mixed inhibitor/activator of histone acetyltransferase (HAT) activity. The compound inhibits the activity of p300/CBP, but potentiates p300/CBP-associated factor (PCAF) activity. SPV106 also induces S-phase cell cycle arrest and apoptosis in U937 cells.
S9188 STAT1-α/β (699-709) >98% (HPLC), solid  
S4690 STAT4 control peptide trifluoroacetate salt >90% (HPLC), lyophilized powder Positive control peptide for the STAT4 rabbit polyclonal antibody.
SML1108 STF-31 ≥98% (HPLC) STF-31 selectively inhibits the glucose transporter GLUT1 and selectively impairs cancer cell growth of kidney and other types of cancer cells that lack the von Hippel-Lindau (VHL) tumor suppressor protein. Inactivation of VHL increases the activity of hypoxia-inducible factor transcription factor HIF, which in turn stimulates the transcription of genes involved in glucose metabolism, including the GLUT1 gene. VHL-deficient cancer cells, which include about 80% of renal cell carcinomas, are dependent on the high affinity GLUT1 transporter and aerobic glycolysis for ATP production. STF-31 binds directly to the GLUT1 transporter, blocking glucose uptake, resulting in necrosis in VHL-deficient cancer cells, but not in normal cells or cancer cells with intact VHL.
SML0596 Strontium ranelate ≥98% (HPLC) Strontium ranelate is a dual action bone agent (DABA). It inhibits bone resorption and stimulates bone formation, inhibiting osteoclast differentiation while activating gene expression in osteoblasts. While its exact mechanism of action is unknown, one hypothesis is that both anabolic and anti-catabolic activities may involve antagonizing nuclear factor-KB (NF-KB) activation in bone cells. Strontium ranelate has been shown to inhibit the receptor activator of NF-KB ligand (RANKL)-induced nuclear translocation of NF-KB and activator protein-1. Strontium ranelate has been used clinically for the treatment of osteoporosis and a recent multinational study indicates the drug can also be used to treat osteoarthritis.
SML1136 SW155246 ≥98% (HPLC) SW155246 is a potent and selective DNMT1 (DNA methyltransferase 1) inhibitor that demethylates cytosines in vivo in a cell-based assay without affecting protein levels or generating reactive oxygen species. SW155246 induces re-expression of the tumor suppressor geneRASSF1 in A549 cells.
SML1894 SYP-5 ≥98% (HPLC) New SYP-5 is potent and selective inhibitor of HIF-1 activity that decreases HIF-1α and HIF-1β protein levels under hypoxic condition. SYP-5 inhibits tumor cell migration and invasion, as well as tumor angiogenesis.
SML1539 TDFA trifluoroacetate salt ≥98% (HPLC) TDFA (Thr-Asp-F-amidine) is a selective inhibitor of peptidyl arginine deiminase 4 (protein arginine deiminase 4, PAD4 or PADI4), a transcriptional coregulator that catalyzes the calcium-dependent conversion of specific arginine residues in proteins to citrulline, a process called citrullination. PAD4 is upregulated in cancer and inflammatory diseases, and may be involved in rheumatoid arthritis onset and progression. It has recently been found to be involved in the regulation of pluripotency: important for stem-cell gene activation, induced pluripotent stem (iPS) cell reprogramming, and maintenance of pluripotent cells in the early mouse embryo. TDFA has an IC50 value of 2.3 μM and is ≥15-fold selective for PAD4 versus PAD1 and ≥50-fold selective versus PADs 2 and 3.
T3455 Terameprocol ≥98% (HPLC) Terameprocol is a synthetic derivative of NDGA, a non-selective lipoxygenase inhibitor. It inhibits Sp1 transcription factor binding at the HIV long terminal repeat promoter and at the α-ICP4 promoter, a gene essential for HSV replication, with IC50 values of 11 and 43.5 μM respectively. TMNDGA induces growth arrest and apoptosis by suppressing Sp1-dependent Cdc2 and survivin gene expression giving rise to its antitumorigenic activity. The in vivo growth of xenografts in numerous human tumor types was suppressed upon treatment with TMNDGA It also inhibits the growth of murine and human melanomas and human colon cancer in vivo without causing other tissue toxicity.
Terameprocol is known to reduce angiogenesis1.
SML1849 TP-064 TFA salt ≥98% (HPLC) TP-064 is a selective chemical probe for protein arginine methyltransferase 4 (PRMT4) developed out of a collaborative effort by Takeda and the SGC. TP-064 inhibited PRMT4 with an IC50 value < 10 nM for methylation of H3 (1-25). It showed greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, TP-064 inhibited the methylation of MED12 with an IC50 value of 43 nM. For full characterization details, please visit the TP-064 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
T6205 TPh A ≥98% (HPLC) TPh A is an inhibitor of the nuclear protein pirin. TPh A (Triphenyl compound A) inhibits the interaction between Bcl3 oncoprotein and the nuclear protein pirin. TPh A inihibits melanoma cell migration.
T2580 Trapoxin A ≥98% (HPLC), from Helicoma ambiens Trapoxin A is a cyclotetrapeptide and a histone deacetylase (HDAC) inhibitor. It increases the level of chromatin acetylation associated with histone H3 at low nanomolar concentrations. Unlike the reversible HDAC inhibition induced by TCA, Trapoxin A irreversibly inhibites HDAC activity in crude cell lysates, and induces the accumulation of hyperacetylated core histones in a number of mammalian cell lines and tissues. Histone acetylation and methylation have been studied extensively for their anti-tumor activities in carcinogenesis and Trapoxin has been suggested as a potential anticancer agent for pre-clinical trials.
T1945 Trichodion >95%, solid Trichodion is a bioactive pyrone that can be isolated from the fungus Trichosporiella sp. Studies have reported that this pyrone can block IFN-γ mediated reporter gene expression in HeLa S3 cells.
T8552 Trichostatin A ≥98% (HPLC), from Streptomyces sp. Inhibits histone deacetylase at nanomolar concentrations; resultant histone hyperacetylation leads to chromatin relaxation and modulation of gene expression. May be involved in cell cycle progression of several cell types, inducing cell growth arrest at both G and G/M phases; may induce apoptosis. Enhances the efficacy of anticancer agents that target DNA.
T1952 Trichostatin A, Ready Made Solution 5 mM in DMSO (0.2 μm-filtered), from Streptomyces sp. Trichostatin A (TSA) is a Streptomyces metabolite, which specifically inhibits mammalian histone deacetylase at a nanomolar concentration and causes accumulation of highly acetylated histone molecules in mammalian cells. For that reason, trichostatin A is a tool to study the consequences of histone acetylation in vivo. Trichostatin A induces cell differentiation, cell cycle arrest, reversal of transformed cells morphology, and apoptosis and is able to modulate transcription. TSA has been used to establish a new cloning technique, which increases the success rates for mouse cloning.
SML0065 Tubacin ≥98% (HPLC) Tubacin is a selective inhibitor of histone deacetylase 6 (HDAC6), a predominantly cytoplasmic class II histone deacetylase that is involved in many cellular processes, including degradation of misfolded proteins, cell migration, and cell-cell interaction. Tubacin selectively inhibit HDAC6-mediated alpha -tubulin deacetylation.
Tubacin triggers the release of reactive oxygen species and mediates caspase-3-independent apoptosis of Epstein-Barr virus (EBV)-positive Burkitt lymphoma cells. It suppresses the proliferation of acute lymphoblastic leukemia (ALL) cells and enhances the effect of chemotherapy to treat ALL cells. Tubacin prevents the epileptic activity and neuronal migration defects caused due to lowered expression of Srpx2 in rats.
SML0044 Tubastatin A hydrochloride ≥98% (HPLC) Tubastatin A increases the total numbers of mitochondria and restores the number of moving mitochondria in DRG neurons. It reverses the axonal loss in peripheral neurons in mouse model of Charcot-Marie-Tooth disease. Tubastatin A inhibits the deacetylation of α-tubulin in murine myoblasts.
Tubastatin A is a very selective HDAC6 inhibitor with an IC50 of 4 nM and 100 to over 1000-fold selectivity for HDAC6 over other HDAC classes.
SML1431 UF010 ≥98% (HPLC) UF010 is a potent class I HDAC (HDAC1, HDAC2, HDAC3, and HDAC8) selective inhibitor that suppresses cancer cells proliferation through class I HDAC inhibition of oncogenic signaling and activation of tumor suppression pathways.
SML1465 UNC0379 trifluoroacetate salt ≥98% (HPLC) UNC0379 is the first substrate-competitive inhibitor of the lysine methyltransferase SETD8, the only known methyltransferase that catalyzes monomethylation of histone H4 lysine 20 (H4K20). HK420 methylation has been implicated in the regulation of a variety of biological processes including the DNA damage response. UNC0379 is selective for SETD8 over 15 other methyltransferases, with an IC50 value of 7.3 μM for SETD8 compared to IC50 vlaues over 100 μM for other methyltransferases.
U4885 UNC0638 hydrate ≥98% (HPLC) UNC0638 hydrate is a histone methyltransferase (HMT) inhibitor. UNC0638 shows selectivity for G9a (EHMT2) and GLP (EHMT1) methyltransferases, which catalyze the methylation of lysine 9 of histone 3 (H3K9) as well as other non-histone substrates. For full characterization details, please visit the UNC0638 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1037 UNC0642 ≥98% (HPLC) UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), which catalyze the mono and dimethylation of lysine 9 of histone 3 (H3K9), and other non-histone substrates such as p53 and WIZ. UNC0642 has an in vitro IC50 <15 nM with greater than 100-fold selectivity over 13 other HMTs and selected representatives of kinases, ion channels, 7TMs, and other epigenetic proteins. UNC0642 has the same potency with improved PK properties relative to UNC0638, which should make it a more useful probe in an in vivo setting. For full characterization details, please visit the UNC0642 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML0633 UNC0646 ≥98% (HPLC) UNC0646 is potent, selective inhibitor of the methyltransferase G9a, which catalyzes lysine-methylation of histones, and nonhistone proteins including p53.
SML0778 UNC1999 ≥98% (HPLC) The polycomb repressive complex 2 (PRC2), which represses gene expression through methylation of histone H3 on lysine 27 (H3K27), contains either EZH1 or EZH2 as its catalytic subunit, with EZH1 being found in both dividing and non-dividing cells, whereas EZH2 is only found in actively dividing cells. UNC1999 is an orally bioavaliable selective inhibitor of both EZH2 and EZH1 lysine methyltransferases with IC50 < 10 nM for EZH2 and 45 nM for EZH1. UNC1999 potently inhibited both wild-type and mutant Y641N EZH2 methyltransferase activity with less than a 5-fold difference in potency, and selectively killed diffused large B cell lymphoma (DLBCL) cells bearing Y641 point mutations. It was selective for EZH2 and EZH1 over 15 other lysine, arginine and DNA methyltransferases. UNC1999 is competitive with the cofactor S-adenosylmethionine (SAM) and non-competitive with the peptide substrate. Because it inhibits both EZH2 and EZH1, UNC1999 has potential advantages over EZH2 selective inhibitors in the disease settings where both PRC2 – EZH2 and PRC2 – EZH1 contribute to the methylation of H3K27. For full characterization details, please visit the UNC1999 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML0011 VAHA ≥98% (HPLC) Hydroxamic acid derivatives of valproic acid exhibit anticonvulsant activity with no teratogenic activity in mouse neural tube defect model. It is effective in the treatment of bipolar disorders.
VAHA (Valproyl hydroxamic acid) is an HDAC inhibitor with less activity than valproic acid against Class I enzymes but much greater Class II activity
SML0859 WDR5-0103 ≥98% (HPLC) WDR5-0103 is a WD40-repeat antagonist that binds to WDR55 central cavity. WDR5-0103 inhibits MLL1 histone methyltransferase activity in vitro through disruption of the interaction of MLL with WDR5.
SML0760 WIKI4 ≥98% (HPLC) WIKI4 is a potent inhibitor of Wnt/β-catenin signaling with an EC50 ~ 75 nM in all cell lines tested including DLD1 colorectal cancer cells, NALM6 B cells, U2OS osteosarcoma cells, and hESCs. WIKI4 inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) with an IC50 of 15 nM, preventing the ubiquitination and degradation of axin and thereby antagonizing Wnt signalling.
SML0899 Windorphen ≥98% (HPLC) Windorphen is a selective Wnt/β-catenin signaling inhibitor acting through selective inhibition of p300, a histone acetyltransferase (HAT) that also acts as a critical coactivator of β-catenin, a transcription factor that mediates the Wnt signaling pathway involved in embryogenesis and cancer cell survival. Windorphen blocks Wnt signaling by selectively disrupting the association of p300 with the C-terminal transactivation domain of β-catenin-1. Windorphen does not inhibit the closely related CREB-binding protein (CBP). Windorphen induced apoptosis in several Wnt-dependent tumor cell lines including colon adenocarcinoma SW480and RKO and prostate cancer cell lines DU145 and PC3.
W4013 WP900 hydrochloride ≥95% (HPLC), solid Synthetic left-handed enantiomer of (+)-daunorubicin, anti-tumor antibiotic, binds to right-handed B-form DNA under low salt conditions.
SML0758 WS3 ≥98% (HPLC) WS3 is a non-cell specific proliferative molecule, thought to act primarily through modulating the activity of ErbB3-binding protein 1 (EBP1) also known as proliferation-associated protein 2G4 (PA2G4), an RNA-binding protein that is involved in growth regulation and inhibition. It may alsohae some activity through the I?B kinase pathway. WS3 was initially found to be a proliferative molecule for β-cells, but more recently found to mediate proliferation of primary retinal pigment epithelial cells. After W3 removal, the retinal cells differentiated into a functional monolayer and remained functional in vivo, preserving vision when they were transplanted into RCS rats used as a model of retinal degeneration.
SML0757 WS6 ≥98% (HPLC) WS6 is an inducer of β cell proliferation, thought to act primarily through modulating the activities of the IKB kinase pathway and ErbB3-binding protein 1 (EBP1) also known as proliferation-associated protein 2G4 (PA2G4), an RNA-binding protein that is involved in growth regulation and inhibition.
SML0621 WZB-117 ≥98% (HPLC) WBZ 117 is an inhibitor of basal glucose transport in H1299 lung and other cancer cells.
X3004 XAV939 ≥98% (HPLC) XAV939 is a Tankyrase inhibitor (thereby inhibiting Wnt / β-catenin signaling)
SML1840 YK-3-237 YK-3-237 is an activator of sirtuin-1 (SIRT1). YK-3-237 showed anti-proliferative activity toward triple-negative breast cancer, inducing G2/M cell cycle arrest and apoptosis. In a study on renal fibrosis, YK-3-237 caused enhanced expression of α-SMA and fibronectin, suggesting that long-term use of SIRT1 activators may increase the risk or progression of chronic kidney disease.