| A1410 | Actinomycin D from Streptomyces sp., ~98% (HPLC) | An antineoplastic antibiotic that inhibits cell proliferation by forming a stable complex with DNA and blocking the movement of RNA polymerase which interferes with DNA-dependent RNA synthesis. Induces apoptosis. Potent antitumor agent. For cell culture applications, actinomycin D is used as a selection agent and is used in banding techniques to differentiate between different regions of chromosomes.
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| A9415 | Actinomycin D from Streptomyces sp., suitable for cell culture, ≥95% | An antineoplastic antibiotic that inhibits cell proliferation by forming a stable complex with DNA and blocking the movement of RNA polymerase which interferes with DNA-dependent RNA synthesis. Induces apoptosis. Potent antitumor agent. For cell culture applications, actinomycin D is used as a selection agent and is used in banding techniques to differentiate between different regions of chromosomes.
Mode of Action: Complexes with DNA and interferes with RNA synthesis.
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| A4262 | Actinomycin D from Streptomyces sp., ~95% (HPLC) | An antineoplastic antibiotic that inhibits cell proliferation by forming a stable complex with DNA and blocking the movement of RNA polymerase which interferes with DNA-dependent RNA synthesis. Induces apoptosis. Potent antitumor agent. For cell culture applications, actinomycin D is used as a selection agent and is used in banding techniques to differentiate between different regions of chromosomes.
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| A8231 | AGK2 ≥97% (HPLC), solid | 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.
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| 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.
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| 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.
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| 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.
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| A8236 | AN-9 ≥95% (HPLC) | HDAC Inhibitor tested as an anti-cancer drug; butyric acid pro-drug
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| A7236 | Anacardic acid ≥98% (HPLC) | Anacardic acid is a HAT (Histone Acetyltransferase) inhibitor.
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| A8851 | Apicidin ≥98% (HPLC), from microbial | Potent (nM) cell permeable inhibitor of histone deacetylase. Also, exhibits antiprotozoal and potential antimalarial properties. Apicidin has antiproliferative activity on HeLa cells accompanied by cell arrest at the G1 phase. In addition, it induces selective changes in the expression of p21 and gelsolin.
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| B4061 | BATCP ≥98% (HPLC), solid | HDAC 6 selective substrate (over HDAC 1, Class II over Class I).
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| 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.1
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| B5313 | BIX-01338 hydrate ≥98% (HPLC) | BIX-01338 is a non-selective histone lysine methyltransferase inhibitor.
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| 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.
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| SML0113 | Brequinar sodium salt hydrate ≥97% (HPLC)  | 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).
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| SML0027 | Butyrylhydroxamic 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.
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| 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.
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| SML0067 | 5-Carboxy-8-hydroxyquinoline ≥97% (HPLC) | 5-Carboxy-8-hydroxyquinoline is a Histone Demethylase Inhibitor. It inhibits the JMJD2 (KDM4) family of 2-oxoglutarate-dependent histone demethylases and binds at the same site as N-oxalyl glycine.
Histone Demethylase Inhibitor
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| C1494 | Carmofur ≥98% (HPLC), powder | Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent.
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| 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.
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| 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.
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| C8742 | CHIC-35 ≥97% (chiral, HPLC), solid | 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.
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| PZ0130 | CP-64434 hydrate ≥98% (HPLC) | CP-064434 is an antibiotic; anti-proliferative HDAC inhibitor.
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| 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.
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| 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.
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| D5816 | (−)-Depudecin >95% (HPLC), from microbial | Inhibitor of histone deacetylase (HDAC) both in vivo and in vitro. Alters the spindle shaped morphology of v-Ha-ras-transformed NIH3T3 cells to a flattened shape and induces an intricate actin stress fiber network in these cells and in MG63 osteosarcoma cells. Also exhibits anti-angiogenic activity.
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| D1916 | 5,6-Dichlorobenzimidazole 1-β-D-ribofuranoside | Inhibitor of RNA synthesis; causes premature termination of transcription. CK2 (casein kinase-2) inhibitor.
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| D2629 | 6-(Dimethylamino)purine ≥98% | | |
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| D6071 | Diphenylacetohydroxamic acid ≥98% (HPLC) | Diphenylacetohydroxamic acid is a class IIa selective histone deacetylase inhibitor.
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| 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.
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| D4071 | 5, 15-DPP | 5, 15-DPP is a selective STAT3 inhibitor and a selective STAT3-SH2 antagonist
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| D6321 | Droxinostat ≥98% (HPLC) | Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8.
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| 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.
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| E4143 | (−)-Epigallocatechin gallate ≥95%, from green tea | Antioxidant polyphenol flavonoid that inhibits telomerase and DNA methyltransferase. EGCG blocks the activation of EGF receptors and HER-2 receptors.
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| E4268 | (−)-Epigallocatechin gallate ≥80% (HPLC), from green tea | | |
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| E7034 | EX-527 ≥98% (HPLC) | Potent SIRT1 inhibitor, IC50 38 nM. More potent and selective than our current SIRT inhibitors. 200-500-fold more selective for SIRT1 than for SIRT2 or SIRT3. Does not inhibit SIRT4-7, does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. Mentioned in several reviews as well as recent Oncogene paper. EX-527 was identified in a high throughput screen. It is racemic and gives similar results and potency as the active isomer, EX-243, whereas the other isomer (designated EX-242) is inactive.
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| 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.
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| 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.
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| 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.
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| 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).
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| H3416 | HR-73 ≥98% (HPLC) | HR-73 is a splitomycin derivative that is a SIRT1 inhibitor. HR-73 induces p53 hyperacetylation and decreases HIV transcription.
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| 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.
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| SML0106 | N-Hydroxy-4-(1-naphthalenyl)-benzamide ≥98% (HPLC) | N-Hydroxy-4-(1-naphthalenyl)-benzamide is a cell-permeable, potent and selective HDAC8 inhibitor.
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| SML0203 | iCRT14 ≥98% (HPLC) | 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.
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| 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.
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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.
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| 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.
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| J4829 | JFD00244 ≥98% (HPLC), solid | JFD00244 is a SIRT (sirtuin, human silent information regulator) inhibitor.
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| 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.
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| 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.
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| 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.
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| M1824 | MC1568 ≥97% (HPLC) | MC1568 is a selective class II (IIa) histone deacetylas (HDAC II) inhibitor.
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| 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.
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| M2195 | MOCPAC ≥95% (HPLC), solid | Selective HDAC1 substrate (over HDAC6, class I over class II).
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| N3289 | N2-Ethyl-2′-deoxyguanosine ≥98% (HPLC), solid | | |
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| SRP3119 | NANOG human recombinant, expressed in Escherichia coli, ≥98% (SDS-PAGE), ≥98% (HPLC), cell culture tested | Nanog is a regulatory protein that is associated with undifferentiated pluripotent cells. Recombinant human Nanog is a 34.7 kDa protein, which is synthesized as a 304 amino acid polypeptide lacking a signal sequence for secretion.
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| SRP3120 | NANOG TAT human recombinant, expressed in Escherichia 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.
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| 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.
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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.
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| M0688 | Pedibin precursor peptide >92% (HPLC), solid | | |
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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.
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| P0083 | PRMT1 from rat recombinant, expressed in Escherichia 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.
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| P9391 | Procainamide hydrochloride | Inhibits DNA methyltransferase and modulates epigenetic regulation of gene expression. Na+ channel blocker and Class IA anti-arrhythmic.
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| P5874 | PTACH ≥98% (HPLC), solid | HDAC inhibitor; more potent than the majority of HDAC inhibitors except for SAHA (gold standard).
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| 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.
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| 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.
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| 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.
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| R9407 | RM-65 ≥98% (HPLC) | RM-65 is an arginine methyltransferase inhibitor and is cell (HepG2) permeable. The compound is not selective between human and fungal PRMT, unlike AMI-1 (CLIC 2931).
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| 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.
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| SML0061 | SAHA ≥98% (HPLC) | 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.
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| 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).
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| S6907 | α-Sarcin from Aspergillus giganteus ≥95% (SDS-PAGE), lyophilized powder | RNase that inactivates the 60S ribosomal subunit.
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| S7817 | Scriptaid ≥95% (H-NMR), solid | Histone deacetylase inhibitor with lower toxicity than trichostatin A; used to enhance protein expression.
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| S8446 | SIRT1 human recombinant, expressed in Escherichia 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 p53.1 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-Lys26.2
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| 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.
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| S3947 | SIRT6 human recombinant, expressed in Escherichia coli, N-terminal histidine tagged, >90% (SDS-PAGE), buffered aqueous glycerol solution | SIRT6 is a nuclear, chromatin-associated protein with an ADP-ribosyltransferase activity. SIRT6 promotes resistance to DNA damage and suppresses genomic instability in mouse cells in association with a role in base excision repair (BER). It has been shown that SIRT6 deficiency in mice leads to the development of an acute degenerative aging-like phenotype. Although SIRT6 is a member of the SIRT family of proteins, it is possible that SIRT6 is not an NAD+ protein deacetylase.1,2
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| S7942 | Sirtinol ≥95% (HPLC) | Sirtinol inhibits yeast Sir2p transcriptional silencing activity in vivo, yeast Sir2p and human SIRT2 deacetylase activity in vitro.
Sirtinol inhibits yeast Sir2p transcriptional silencing activity in vivo, yeast Sir2p, and human SIRT2 deacetylase activity in vitro.
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| S4068 | Splitomicin ≥98% (HPLC), powder | Sir2p (silent information regulator) and HDAC inhibitor.
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| 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.
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| S9188 | STAT1-α/β (699-709) >98% (HPLC), solid | | |
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| S4690 | STAT4 control peptide trifluoroacetate salt >90% (HPLC), lyophilized powder | Positive control peptide for the STAT4 rabbit polyclonal antibody.
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| 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.
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| 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.
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| 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.1 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.2, 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.3
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| T1945 | Trichodion >95%, solid | | |
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| 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.
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| 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.1 Trichostatin A induces cell differentiation, cell cycle arrest, reversal of transformed cells morphology, and apoptosis and is able to modulate transcription.2,3 TSA has been used to establish a new cloning technique, which increases the success rates for mouse cloning.4
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| SML0065 | Tubacin hydrate ≥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.
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| SML0044 | Tubastatin A hydrochloride ≥98% (HPLC) | 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.
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| U4885 | UNC0638 hydrate ≥98% (HPLC) | UNC0638 hydrate is a histone methyltransferase inhibitor (HMT); G9a/GLP selective methyltransferase chemical probe. For full characterization details, please visit the UNC0638 probe summary on the Structural Genomics Consortium (SGC) website.
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| SML0011 | VAHA ≥98% (HPLC) | VAHA (Valproyl hydroxamic acid) is an HDAC inhibitor with less activity than valproic acid against Class I enzymes but much greater Class II activity
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| 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.
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| X3004 | XAV939 ≥98% (HPLC) | XAV939 is a Tankyrase inhibitor (thereby inhibiting Wnt / β-catenin signaling)
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