Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.The chromo and bromo domains, which typically bind acetyllysine, the malignant brain tumor (MBT), the plant homeodomain (PHD), and Tudor domains, which typically associate with methyllysine, are well-known examples of reader domains. The identification of selective inhibitors that specifically target members of the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers has had a significant impact on research on epigenetic readers. 46 proteins, containing 61 bromodomains grouped into eight families, are encoded by the human genome. The first BET inhibitors, GSK 525762A and (+)-JQ-1, are discovered using various experimental methods.
Enhancer of zeste homologue 2 (EZH2), a protein from the Polycomb group (PcG), is crucial for promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This EZH2 function is crucial for cell proliferation, inhibits cell differentiation, and may contribute to the development of cancer. By phosphorylating EZH2, cyclin-dependent kinases control epigenetic gene silencing. Tumor suppressor genes are thought to be silenced by abnormal histone and DNA methylation caused by EZH2 in many cancer types, including lymphomas and leukemia.
In addition to acting as a transcriptional adaptor, p300/CBP also acts as a histone acetyltransferase.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V4552 | GNE-272 | 1936428-93-1 | GNE-272 is a novel, potent and selectivein vivochemical probe for and inhibitor of the CBP/EP300bromodomainswithIC50values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. |
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V4553 | GNE-781 | 1936422-33-1 | GNE-781 (GNE781) is a novel, highly potent and selectiveinhibitor of CBP (Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein) with immunomodulatory and anticancer effects. |
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V56146 | GNE-886 | 2101957-05-3 | GNE-886 (Compound 21) is a potent and specific inhibitor of cat eye syndrome chromosome candidate region 2 bromodomain (CECR2, BRD) with IC50 of 0.016 µM and EC50 of 370 nM. |
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V4084 | GSK-5959 | 901245-65-6 | GSK5959 is a novel, potent, selective and cell permeableBRPF1 (bromodomain and PHD finger-containing) bromodomaininhibitor with an IC50 of 80 nM. |
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V79657 | GSK023 | GSK023 (compound 31) is a selective chemical probe targeting the BD1 domain of BET. | |
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V56126 | GSK040 | 2752331-09-0 | GSK040 is a potent and specific BET BD2 inhibitor (antagonist) with pIC50 of 8.3. |
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V52039 | GSK097 | 2159137-02-5 | GSK097 is a potent and specific inhibitor of bromoalkanes and BET protein second bromoalkane (BD2). |
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V0422 | GSK1324726A (I-BET-726) | 1300031-52-0 | GSK1324726A (I-BET726; GSK-1324726A), atetrahydroquinoline analog, is a novel and potent ApoA1 up-regulator and selective BET Bromodomain inhibitor with anticancerand anti-inflammatory activity. |
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V56135 | GSK217 | 2748687-92-3 | GSK217 is a specific, highly soluble inhibitor of the second bromodomain (BD2) of the bromodomain and extracellular domain (BET). |
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V56149 | GSK232 | 2702984-69-6 | GSK232 is a selective cell-penetrating/penetrable CECR2 inhibitor (antagonist) with excellent physical and chemical properties. |
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V0419 | GSK2801 (GSK-2801) | 1619994-68-1 | GSK2801 (GSK-2801) is a novel, orally bioavailable, selective, cell bioactive and acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains,which are the two closely related bromodomain containing proteins BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. |
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V3545 | GSK4028 | 2079886-19-2 | GSK4028 is the enantiomeric isomer and a negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, thepIC50of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay. |
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V2311 | GSK620 | 2088410-46-0 | GSK620 is a potent orally bioactive pan-BD2 inhibitor (antagonist) with good broad spectrum (a wide range) selectivity, developability and in vivo oral pharmacokinetics, and is selective for BET-BD2 family proteins, exceeding all other BETs bromodomains 200 times more. |
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V2764 | GSK6853 | 1910124-24-1 | GSK6853 is a novel, potent and selective benzimidazolone BRPF1 bromodomain inhibitor with pIC50 of 8.1 (TR-FRET) and showed greater than 1600-fold selectivity over all other bromodomains tested. |
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V56148 | GSK737 | 2748687-95-6 | GSK737 is a BRD4 BD1 and BD2 inhibitor (antagonist) with pIC50s of 5.3 and 7.3 respectively. |
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V76953 | GSK761 | GSK761 is a selective inhibitor of Sp 140 nuclear body protein (SP140) with IC50 of 77.79 nM. | |
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V56125 | GSK852 | 2305842-30-0 | GSK852 is a very potent BD2-selective BET inhibitor (pIC50 = 7.9). |
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V2727 | GSK9311 | 1923851-49-3 | GSK9311 is an analog of GSK-6853, which is a benzimidazolone analog and a novel potent and highly selective inhibitor of the BRPF1(Bromodomain and PHD Finger-containing) bromodomain withmicromolar activity in a cellular target engagement assay, itshows excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested. |
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V0412 | I-BET151 (GSK1210151A) | 1300031-49-5 | I-BET151 (also known as GSK-1210151A) is a novel, potent and selective BET (Bromodomain and extra terminal domain) inhibitor with anticancer activity. |
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V51959 | I-BET151 dihydrochloride (GSK1210151A dihydrochloride) | 1883545-47-8 | I-BET151 di-HCl (GSK1210151A di-HCl) is a BET bromodomain inhibitor, inhibiting BRD4, BRD2 and BRD3 with pIC50 of 6.1, 6.3 and 6.6 respectively. |
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