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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V4200 | BAY-1238097 | 1564268-08-1 | BAY-1238097 (the S-isomer of BAY-1238097) is a novel, potent and selective inhibitor ofBET (bromodomain and extra-terminal) binding to histonesand targeting the NFKB/TLR/JAK/STAT signalling pathways, MYC and E2F1-regulated genes, cell cycle regulation and chromatin structure. |
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V4187 | BAY-299 | 2080306-23-4 | BAY-299 (BAY299) is a novel, highly potent, and selective dual inhibitor of BRD1 and TAF1with important biological activity. |
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V4188 | BAY-850 | 2099142-76-2 | BAY-850 is a novel, potent and isoform selective inhibitor of ATPase family AAA domain-containing protein 2(ATAD2)with anIC50of 166 nM. |
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V52361 | BAZ1A-IN-1 | 941521-45-5 | BAZ1A-IN-1 is a potent BAZ1A (bromodomain-containing protein) inhibitor. |
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V77788 | BD-9136 | BD-9136 is a selective BRD4 degrader. | |
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V78405 | BET BD2-IN-1 | BET BD2-IN-1 (compound 45) is a potent and specific inhibitor of BET BD2 (IC50 of 1.6 nM). | |
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V52345 | BET bromodomain inhibitor 3 | 854137-39-6 | BET bromodomain inhibitor 3 is a BET bromodomain inhibitor. |
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V4203 | BET-BAY 002 S enantiomer | 2070009-49-1 | BET-BAY 002 S enantiomer is the S-enantiomer of BET-BAY 002 which is a novel and potentBET(Bromodomainand extra-terminal) inhibitor. |
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V75499 | BET-IN-1 | 2727161-43-3 | BET-IN-1 is a potent BET inhibitor (antagonist) with good brain penetration and reasonable metabolic stability. |
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V51051 | BET-IN-13 | 2506823-08-9 | BET-IN-13 is a potent BET template with IC50 of 1.6 nM. |
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V52344 | BET-IN-14 | 2243669-93-2 | BET-IN-14 is an orally bioactive pan-BET inhibitor (IC50= 5.35 nM). |
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V52343 | BET-IN-15 | 2408994-22-7 | BET-IN-15 (compound 1) is a potent and orally bioactive BET inhibitor (antagonist) with IC50s of 0.64 and 0.25 nM for BRD4-BD1 and BRD4-BD2, respectively. |
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V56147 | BET-IN-16 | 2089390-09-8 | BET-IN-16 (Comp I) is a BET inhibitor. |
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V78301 | BET-IN-17 | BET-IN-17 (compound 16) is a pan-inhibitor of BET with pIC50s of 7.8 and 7.6 for BET BD1 and BET BD2, respectively. | |
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V56140 | BET-IN-19 | 1643947-30-1 | BET-IN-19 (Compound 146) is a BET inhibitor. |
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V75503 | BET-IN-20 | 1300735-76-5 | BET-IN-20 (compound 10) is an inhibitor (blocker/antagonist) of BRD4 BD1 (IC50=1.9 nM) and has anti-neoplastic activity. |
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V75495 | BET-IN-6 | 2570470-39-0 | BET-IN-6 is a potent and high-affinity BRD2/BRD4 inhibitor. |
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V75504 | BET-IN-8 | 2769893-19-6 | BET-IN-8 (Compound 27) is a potent BET inhibitor (antagonist) with Ki and Kd< /sub> of 0.83 and 0.571 μM, respectively. |
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V3578 | BETd-246 | 2140289-17-2 | BETd-246 is a novel, potent and second-generationBET bromodomain (BRD)degrader which exhibits superior selectivity, potency and antitumor activity. |
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V4705 | BI-7273 | 1883429-21-7 | BI-7273 is a novel, potent, selective, and cell-permeableBRD9inhibitor with IC50and Kdof 19 and 0.75 nM, respectively; it also shows high effect on BRD7 with IC50and Kdof 117 nM and 0.3 nM, respectively. |
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