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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V51958 | I-BET282E | 2885162-99-0 | I-BET282E is a pan-inhibitor of eight BET bromodomains with selectivity for other representative alkyl bromide-containing proteins. |
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V80125 | I-BET432 | I-BET432 is a BET inhibitor. | |
|
V51957 | I-BET567 | 1887237-54-8 | I-BET567 is a potent, orally bioactive pan-BET inhibitor candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. |
|
V33303 | I-BET762 carboxylic acid | 1300019-38-8 | I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. |
|
V22379 | I-BRD9 | 1714146-59-4 | I-BRD9 is a BRD9 specific inhibitor, identified by scientists at GlaxoSmithKline. |
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V56155 | I-CBP112 hydrochloride | 2147701-33-3 | I-CBP112 HCl is a selective CBP/P300 inhibitor that binds directly to their bromodomain (Kds of 142 and 625 nM, respectively). |
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V22368 | IACS-9571 | 1800477-30-8 | IACS-9571 is a novel, potent and selective TRIM24 and BRPF1 inhibitorwithIC50value of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively. |
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V51960 | IACS-9571 hydrochloride (ASIS-P040 hydrochloride) | 2319611-93-1 | IACS-9571 (ASIS-P040) HCl is an inhibitor (blocker/antagonist) of bromodomain proteins TRIM24 and BRPF1. |
|
V51956 | iBRD4-BD1 | 2839318-17-9 | iBRD4-BD1 is a selective BRD4 bromodomain inhibitor. |
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V3808 | INCB054329 | 1628607-64-6 | INCB054329 is a novel potent and selective inhibitor ofBromodomain and extra-terminal (BET) protein. |
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V3764 | INCB057643 | 1820889-23-3 | INCB057643 is a novel, orally bioavailable BET inhibitor that has been tested in preclinical models of hematologic malignancies. |
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V31532 | Inobrodib (CCS1477) | 2222941-37-7 | Inobrodib (CCS1477;BP-IN-1; CCS-1477) is a novel, potent and selective p300/CBP bromodomain inhibitor with anticancer activity. |
|
V76877 | IV-255 | IV-255 is a selective small molecule inhibitor of the BRG1 bromodomain. | |
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V79949 | IV-275 | IV-275 is an inhibitor (blocker/antagonist) of BRG1 and BRM bromodomains. | |
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V51917 | JQ1-TCO | 2087490-43-3 | JQ1-TCO (JQ1-trans-cycloctene) is an analogue of the BET inhibitor JQ1 . |
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V51908 | KB02-JQ1 | 2384184-44-3 | KB02-JQ1 is a selective PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. |
|
V3685 | KG-501 | 18228-17-6 | KG-501 is a potent inhibitor of CREB (cAMP response element-binding protein)with anIC50of 6.89 μM. |
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V76815 | L-Moses dihydrochloride (L-45 dihydrochloride) | L-Moses (L-45) di-HCl is the first potent and specific p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor (antagonist) with a Kd of 126 nM. | |
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V51831 | M-1211 | 2377337-93-2 | M-1121 is a covalent and orally bioactive inhibitor of the menin-MLL interaction that achieves complete and durable tumor regression. |
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V52927 | Menin-MLL inhibitor 19 | 2360487-93-8 | Menin-MLL inhibitor 19, a potent inhibitor of menin-mll interaction, Example A17, originated from patent WO2019120209A1. |
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