| A1705 | S-(5′-Adenosyl)-L-homocysteine Hydrolase from rabbit erythrocytes buffered aqueous glycerol solution, ≥10 units/mg protein (Lowry) | Enzyme in vertebrates which catabolizes S-adenosyl-L-homocysteine.
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| SML0009 | AI-1 ≥98% (HPLC) | AI-1 promotes Nrf2 activation via the covalent modification of Kelch-like ECH-associated protein 1 (Keap1), a negative regulator of Nrf2. Biochemical studies indicate that an aromatic chloride present within the AI-1 molecule undergoes a nucleophilic aromatic substitution reaction with cysteine thiols of Keap1.
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| A9232 | AMI-1 sodium salt hydrate ≥98% (HPLC) | Protein arginine N-methyltransferases (PRMTs) are involved in post-translational modification implicated in protein trafficking, signal transduction, and transcriptional regulation. AMI-1 does not inhibit lysine methyltransferase activity and does not interact with S-adenosylmethionine (AdoMet), unlike most methyltransferase inhibitors which compete for the AdoMet binding site. AMI-1 can modulate nuclear receptor-regulated transcription from estrogen and androgen response elements; and is a HIV-1 reverse transcriptase inhibitor. AMI-1 is a potent antagonist of NADPH-oxidase-derived superoxide production, but acts as a direct antioxidant rather than indirectly through methyltransferase inhibition.1
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| A0987 | n-Amyl 2-[3,5-dihydroxy-2-(1-nonanoyl)phenyl]acetate ≥98% (HPLC) | n-Amyl 2-[3,5-dihydroxy-2-(1-nonanoyl)phenyl]acetate is a Nur77 agonist. Nur77 is a steroid orphan receptor that plays a critical role in regulating proliferation, differentiation and apoptosis. n-Amyl 2-[3,5-dihydroxy-2-(1-nonanoyl)phenyl]acetate, a cytosporone B analog, is a stronger activator of Nur77 than it parent compound. n-Amyl 2-[3,5-dihydroxy-2-(1-nonanoyl)phenyl]acetate treatment causes Nur77 migration to mitochondria, which results in mitochondrial Cyt c release into the cytoplasm and mitochondrial AIF redistribution in both the cytoplasm and nucleus.
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| SML0104 | Ascochlorin ≥98% (HPLC), from Verticillium hemipterigenum  | Ascochlorin is an isoprenoid antibiotic produced by Verticillium hemipterigenum, initially identified as an antiviral and antitumor agent. Research also indicates that ascochlorin inhibits the Qi and Qo quinone binding sites of the mitochondria cytochrom bc1 complex.1 Moreover, ascochlorin activates p53, probably as a result of its inhibitory effect on mitochondrial respiration.2, In addition, ascochlorin has the ability to suppress the nuclear subscription enzyme protein-1, a nuclear transcription factor activator, which leads to suppression of the extra-cellular enzyme, matrix metalloproteinase-9 (MMP9).3, The regulation of MMP is implicated in renal development, macrophage differentiation, atherosclerosis, inflammation, rheumatoid arthritis, and tumor invasion. Ascochlorin was also found to be effective against Mx-1, an estrogen lacking breast cancer cell line.4
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| A2385 | 5-Azacytidine ≥98% (HPLC) | A potent growth inhibitor and cytotoxic agent; inhibits DNA methyltransferase, an important regulatory mechanism of gene expression, gene activation and silencing.
Causes DNA demethylation or hemi-demethylation, creating openings that allow transcription factors to bind to DNA and reactivate tumor suppressor genes.
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| A3656 | 5-Aza-2′-deoxycytidine ≥97% | 5′-Azadeoxycytidine causes DNA demethylation or hemi-demethylation. DNA demethylation can regulate gene expression by "opening" the chromatin structure detectable as increased nuclease sensitivity. This remodeling of chromatin structure allows transcription factors to bind to the promoter regions, assembly of the transcription complex, and gene expression.
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| B5556 | Bay 11-7082 ≥98% (HPLC), powder | Bay 11-7082 is an inhibitor of cytokine-induced IκB-α phosphorylation.
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| B5681 | Bay 11-7085 ≥98% (HPLC), solid | Inhibits NF-κB activated expression of ICAM-1, VCAM-1, E-selectin, IL-6 and IL-8.
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| B9061 | Bicalutamide (CDX) ≥98% (HPLC), powder | Bicalutamide (CDX) is a non-steriodal Androgen Receptor (AR) antagonist and a pure antiandrogen. It acts via balancing histone acetylation/deacetylation and recruitment of coregulators. Bicalutamide (CDX) abolishes androgen-mediated expression. For example, MMP13 upregulation in prostate cancer, PLZF (promyelocytic leukemia zinc finger protein), and GADD45γ (growth arrest and DNA damage inducible, gamma). Bicalutamide (CDX) is inhibited by non-genomic, transcription-independent stimulation of PI3K/AKT phosphorylation by androgens.
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| B7563 | BRD7389 ≥98% (HPLC) | BRD7398 is a RSK kinase inhibitor that induces insulin expression and differentiation of pancreatic alpha into beta cells. BRD7398 inhibits RSK1, RSK2 and RSK3; IC50 values of 1.5, 2.4 and 1.2 uM, respectively. Treatment of mouse aTC1 cells with BRD7398 induced expression of b-cell markers Pdx1, Pax4, Iapp and Npy and also induced insulin production.
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| C8221 | Caffeic acid phenethyl ester ≥97% (HPLC), powder | Caffeic acid phenethyl ester is a specific inhibitor of the nuclear transcription factor NF-κB.
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| C4369 | Calcipotriol hydrate ≥99% (HPLC) | Calcipotriol, a synthetic derivative of calcitriol or Vitamin D, is used in the treatment of psoriasis and marketed under the trade name Dovonex. It has comparable affinity with calcitriol (Vit. D) for the Vitamin D receptor (VDR), while being less than 1% as active as the calcitriol in regulating calcium metabolism. VDR belongs to the steroid/thyroid receptor superfamily, and is found on the cells of many different tissues including the thyroid, bone, kindney, and T cells of the immune system. Binding of calcipotriol to the VDR modulates the T cells gene transcription of cell differentiation and proliferation-related genes.
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| C0494 | Cambinol ≥97% (HPLC), white powder | Cambinol is a Sirtuin (Human Silent Information Regulator) Type 1/2 Inhibitor. Sirtuins are structurally and mechanistically unrelated to HDACs Class 1 & 2 deacetylases but share many protein targets. HDAC is a large complex enzyme family involved in epigenetic-control of gene expression. Sirt2 has an IC50 equal to 59 μM.
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| C1357 | Cholecalciferol meets USP testing specifications | Vitamin D acts through a receptor that is a member of the ligand-dependent transcription factor superfamily. Modulates the proliferation and differentiation of both normal and cancer cells. Has antiproliferative and antimetastatic effects on breast, colon, and prostate cancer cells. Activated vitamin D receptors in intestine and bone maintain calcium absorbance and homeostasis.
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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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| C2997 | Cytosporone B ≥98% (HPLC) | Cytosporone B (Csn-B) is the first naturally occurring agonist for nuclear orphan receptor Nur77. It binds with high affinity (IC50=0.278 nM) to the ligand-binding domain of Nur77 and stimulates Nur77-dependent activities.
Nur77 is a nuclear receptor/transcription factor. A physiological ligand for Nur77 is as yet unknown, but there is increasing interest in Nur77 because of its known activities. Translocation of Nur77 from the nucleus to mitochondria initiates cell apoptosis, making it a potential target for cancer treatment. Nur77 is also involved in glucose homeostasis; it induces genes involved in gluconeogenesis. Csn-B physically binds to Nur77 and activates its transactivational activity and translocation to mitochondria to induce apoptosis. It inhibits cancer cell proliferation and tumor growth.
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| D9568 | 3,3′-Diindolylmethane ~98% (HPLC) | Acid-catalyzed reaction product of a phytochemical naturally found in Brassicaceae, indole-3-carbinol.1 It functions as an antitumor agent. This derivative can both directly stimulate apoptosis at relatively high concentrations and sensitize TRAIL-induced apoptosis in human cancer cells.2,3 DIM induces a G1 cell cycle arrest in human breast cancer MCF-7 cells by a mechanism that includes increased expression of p21. DIM is a strong mitochondrial H+-ATPase inhibitor.4 The function of DIM and its derivatives as a new plant growth promoter has been studied in an eco-friendly system.5
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| SML0079 | DiMNF ≥98% (HPLC) | DiMNF is a naphthoflavone derivative, selective aryl hydrocarbon receptor modulator (SAhRM). DiMNF is an AHR ligand that does not induce the expression of AHR dependent genes, such as CYP1A1, but inhibits the expression of cytokine-induced acute phase response proteins such as serum amyloid A and complement C3.
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| D7946 | DIM-C-pPhOCH3 ≥98% (HPLC) | DIM-C-pPhOCH3 is a Nerve Growth Factor-Induced Bα (NGFI-Bα, Nur77) agonist
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| D0196 | Doxercalciferol ≥98% (HPLC), solubility: >10 mg/mL in DMSO | Doxercalciferol is a Vitamin D2 analogue, a Vitamin D Receptor Activator (VDRA). Doxercalciferol acts as a pro-hormone, needing 25-hydroxylation in the liver for bioactivation into 1α, 25-hydroxyvitamin D2. Pivotal studies in adults on dialysis have demonstrated control of secondary hyperparathyroidism that is superior to placebo therapy, without undue suppression of 1st IMA-PTH < 300 pg/mL, or occurrences of hypercalcemia. Doxercalciferol has been shown to be effective in controlling secondary hyperparathyroidism of adult patients with CKD stages 3-4.
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| SRP0253 | 4EBP1 Active human recombinant, expressed in Escherichia coli, ≥70% (SDS-PAGE) | | |
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| E8409 | EF-24 ≥98% (HPLC) | EF-24 is a IKK inhibitor and curcumin analog. EF-24 is more potent and bioavailable than curcumin, with 10-fold greater potency in cell death induction. It is also more efficacious in anti-cancer screens and less toxic than Cisplatin. EF-24 inhibits HIF-1alpha posttranscriptional activity and induces microtubule stabilization, in contrast to Curcumin. EF-24 up-regulates PTEN expression via inhibition of ubiquitination. EF-24 induces cell death through direct inhibition of IkappaB kinase (IKK), resulting in suppression in NFκB activity.
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| SRP0255 | eIF4E Active human recombinant, expressed in Escherichia coli, ≥70% (SDS-PAGE) | | |
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| SML0149 | 3-Ethoxy-5,6-dibromosalicylaldehyde ≥95% (HPLC) | 3-Ethoxy-5,6-dibromosalicylaldehyde is a non-competitive inhibitor of Inositol-requiring enzyme 1 (IRE1). It inhibits XBP-1 splicing induced pharmacologically in human cells. 3-Ethoxy-5,6-dibromosalicylaldehyde potently inhibits the endoribonuclease of IRE1 but does not inhibit RNases A, T1, or L.
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| G0673 | GSK4112 ≥98% (HPLC) | GSK4112 is a rev-erbα, (orphan nuclear receptor NR1D1) agonist, the first agent able to reset the circadian clock in a phase-dependent manner. Rev-erbα impacts the precision of the circadian clock by repressing target gene activities with the help of a nuclear receptor co-repressor complex (NCoR) and HDAC3. GSK4112 competes with heme (rev-erb′s natural ligand) and enhances co-repressor complex recruitment and thus, repression of transcription. suggests that pharmacological modulation through Rev-erb may provide new routes to treat metabolic diseases, especially disorders of adipogenesis regulated by rev-erba.1
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| H4014 | 25-Hydroxycholecalciferol ≥98% (HPLC) | | |
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| SML0110 | Ilicicolin F ≥98% (HPLC), from Verticillium hemipterigenum | Ilicicolin F belongs to the ascochlorin family of molecules.1, Ascochlorin is an isoprenoid antibiotic produced by Verticillium hemipterigenum. Ascochlorin and its derivatives have an inhibitory effect on mitochondrial respiration by blocking the oxidation-reduction of cytochrome b through center N of the cytochrome bc1 complex.1,2 Ilicicolins have antiviral activity. They inhibit the growth of the tobacco mosaic virus, herpes simplex virus type-1(HSV-1) and newcastle disease virus.1,2,3
Compounds of the ascochlorin family such as Ilicicolin F, C, D and H show a wide range of inhibitory effects on farnesyl protein transferase (FPTase) activity, and a significant inhibitory effect on the activity of testosterone-5α-reductase.1 Ilicicolin C and F have a moderate inhibitory activity toward the enzymes acetylcholinesterase (AChE) and β-glucuronidase and are active against Pseudomonas syringae with IC50 values of 28.5 μg/mL.1
All isolated ascochlorin analogs exhibit significant antitumor and cytotoxic activities.1,3 Ascochlorin and its homologues are usable in treating and/or preventing diseases that can be relieved by the retinoid X receptor ligand-dependent signal transcriptional regulation (i.e. hypertension, cerebrovascular diseases, rheumatoid arthritis, autoimmune diseases, complication of diabetes, arteriosclerosis etc.). Moreover, they can inhibit denaturation and/or necrosis of pancreatic Langerhans islet β-cells and therefore can sustain insulin productivity.4
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| M6682 | Methoprene acid ≥98% (TLC) | | |
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| N7032 | NFAT Inhibitor >96% (HPLC), solid | High-affinity calcineurin-binding peptide that inhibits NFAT (Nuclear Factor of Activated T cells) activation and NFAT-dependent expression of endogenous cytokine genes in T cells.
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| SML0046 | NSC 668036 hydrate ≥98% (HPLC) | NSC 668036 binds to the PDZ domain of the Wnt-pathway signaling molecule Disheveled (Dvl), blocking the binding and activation of Dvl by Frizzled. In Xenopus embryos, NSC 668036 inhibited Wnt3A-induced expression of the target gene Siamois and formation of secondary axes.
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| O0516 | Oncrasin-1 ≥98% (HPLC) | Oncrasin-1 is a suppressor of RNA processing machinery. Oncrasin-1 induces aggregation of PKCL in the nuclei and is proapoptotic.
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| SAB4200110 | Anti-PIWIL1 (internal region) antibody produced in rabbit ~1.0 mg/mL, buffered aqueous solution | | |
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| SAB4200150 | Anti-PIWIL3 (N-terminal) antibody produced in rabbit ~1.0 mg/mL | | |
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| SRP0190 | RbAp48 Active human recombinant, expressed in baculovirus, ≥40% (SDS-PAGE) | | |
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| R1906 | RETRA ≥98% (HPLC), solid | RETRA is a mutant p53-dependent activator of p73, an activator of p53-regulated genes, and a suppressor of mutant p53-bearing tumor cells. Greater than 50% of tumors express mutant p53 which is defective for the tumor-suppressor function and contributes to malignancy by blocking a p53 family member p73. Activation of p73 in human cancer produces a cytotoxic effect. RETRA increases expression level of p73 and releases p73 from the inhibitory complex with mutant 53. It thereby produces tumor-supressor effect, in vitro and in vivo, similar to functional reactivation of p53.
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| S1323 | SID7969543 ≥98% (HPLC), solid | SID7969543 is a SF-1 (or NR5A1) inhibitor. The Steroidogenic Factor 1 (SF-1, also known as NR5A1) is a transcription factor belonging to the nuclear receptor superfamily. It plays a central role in sex determination and the formation of steroidogenic tissues during development, and is involved in endocrine function throughout life. It has also been reported to have a potential role in obesity. It has also been observed that an increased concentration of SF-1 causes adrenocortical cell proliferation and cancer.
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| S8559 | Sinefungin 95% (HPLC), powder | Sinefungin blocks the methylation of bases in DNA and RNA, such as 5-methylcytosine or N6-methyladenosine, suggesting a role in gene expression. In addition, sinefugin is involved in physiological processes such as aging and carcinogenesis.
Sinefungin blocks the methylation of bases in DNA and RNA, such as 5-methylcytosine or N6-methyladenosine, suggesting a role in gene expression. In addition, sinefugin is involved in physiological processes such as aging and carcinogenesis.
Methylation inhibition by sinefugin is often accompanied by an altered rate of cytosine deamination that is coupled to transition mutation in the DNA. Sinefugin inhibits Epstein-Barr viral activity and this inhibition is related to the change in DNA methylation and gene expression. It can cause a rate change in several restriction DNA endonuclease activities, including Mme I, which is not connected to the inhibition of the methytransferase activity.
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| S9576 | SR8278 ≥98%, semisolid | SR8278 is a Nuclear Heme Receptor REV-ERB antagonist. REV-ERBα plays a critical role in regulation of the circadian rhythm by repressing target gene activities. Additionally, REV-ERBα has been shown to regulate metabolic processes including lipid and glucose metabolism. SR8278 blocks the ability of the synthetic agonist GSK4112 to enhance REV-ERBα-dependent repression and stimulates the expression of REV-ERBα target genes involved in gluconeogenesis.
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| T5202 | TPBM ≥98% (HPLC), solid | TPBM is a potent inhibitor of estrogen receptor α via blocking ERα binding to consensus estrogen response element (cERE) DNA. Estrogen receptor α (ERα) plays an important role in several human cancers. Current ERα antagonists bind in the receptor ligand binding pocket and compete for binding with estrogenic ligands. TPBM instead inhibits ERα via binding to consensus estrogen response element (cERE) DNA. TPBM is not toxic to cells and does not effect estrogen-independent cell growth. TPBM does not act by chelating the zinc in ERs zinc fingers and differs from known ERα inhibitors.
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| T4080 | 6, 2′, 4′-trimethoxyflavone ≥98% (HPLC) | 6, 2′, 4′-trimethoxyflavone is a selective aryl hydrocarbon receptor (AHR) antagonist with no partial agonist activity. The role of the transcription factor aryl hydrocarbon receptor (AHR) in biology is still under evaluation and has expanded beyond that of a xenobiotic sensor and regulator of detoxification. Inhibition of AHR activity by antagonists could result in anti-inflammatory actions. 6, 2′, 4′-trimethoxyflavone (TMF) is a pure AHR antagonist. The compound compete with agonists, such as 2, 3, 7, 8-tetrachlorodibenzo-p-dioxin (TCDD) and benzo[a]pyrene (B[a]P), thus effectively inhibiting AHRmediated transactivation of a heterologous reporter and endogenous targets e.g. CYP1A1. TMF also exhibits no species or promoter dependency with regard to AHR antagonism. Thus it represents an improved tool allowing for more precise dissection of AHR function.
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| Y1646 | YH439 ≥98% (HPLC) | YH439 is an aryl hydrocarbon receptor activator
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