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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V4567 | ABBV-744 | 2138861-99-9 | ABBV-744 (ABBV744) is a novel, potent and highlyBDII-selective BET bromodomaininhibitor with anticancer and anti-inflammatory activity. |
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V52455 | ACBI2 | 2913161-19-8 | ACBI2 is a potent and orally bioactive VHL PROTAC SMARCA2 degrader (EC50= 7 nM) that degrades SMARCA2 (DC50= 1 nM in RKO cells). |
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V56120 | Amredobresib (BI894999) | 1610044-98-8 | Amredobresib is a potent BET inhibitor. |
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V84952 | AR/BET protein degrader-1 | 2571123-81-2 | |
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V3575 | ARV-825 | 1818885-28-7 | ARV-825 (ARV825) is a novel and potent BRD4 degrader based on PROTAC (proteolysis-targeting chimera) technology, anticancer activity. |
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V84395 | ATAD2-IN-1 | 3004556-06-0 | |
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V103553 | ATF4-IN-2 | 2991057-60-2 | ATF4-IN-2 (Compound 29) is an ATF4 inhibitor with IC50 of 47.71 nM. |
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V88852 | AU-24118 | AU-24118 is an orally bioavailable proteolytically targeted chimeric (PROTAC) degrader of mSWI/SNF ATPase (SMARCA2 and SMARCA4) and PBRM1. | |
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V2765 | AZD5153 HNT salt | 1869912-40-2 | AZD-5153 HNT salt, the 6-Hydroxy-2-naphthoic acid salt form of AZD5153, is a potent, selective, and orally available BET/BRD4 (bromodomain and extraterminal) bromodomain inhibitor with pKi of 8.3 for BRD4. |
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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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V86079 | BAY-155 | 2163769-52-4 | |
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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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V88856 | BBC0403 | 2644662-83-7 | BBC0403 is a selective BRD2 inhibitor with Kd of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. |
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V77788 | BD-9136 | 3037514-38-5 | 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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V98401 | BET BD2-IN-3 | 2677039-66-4 | BET BD2-IN-3 (Compound I-58) is a BET inhibitor targeting the BD2 domain of BET. |
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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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V88853 | BET bromodomain inhibitor 4 | 2407658-41-5 | BET bromodomain inhibitor 4 (example 7) is an inhibitor of the BET bromodomain domain. |
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