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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V53049 | (+)-JQ-1-aldehyde | 2634778-37-1 | (+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. |
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V0411 | (+)-JQ1 | 1268524-70-4 | (+)-JQ1 is a novel, potent and highly specific BET (Bromodomain and extra terminal domain) bromodomain inhibitor with antineoplastic activity. |
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V3740 | (+)-JQ1 carboxylic acid | 202592-23-2 | (+)-JQ1 carboxylic acid is the free carboxylic acid (COOH) form of (+)-JQ1 (tert-Butyl ester form-COOtBu). |
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V3741 | (+)-JQ1 PA | 2115701-93-2 | (+)-JQ1 PA (also known as (+)-JQ1 propargyl amide) is a novel propargyl amide derivative of (+)-JQ1 with IC50of 10.4 nM for Bromodomain and extra-terminal(BET). |
|
V77414 | (1s,4s)-Menin-MLL inhibitor-23 | (1s,4s)-Menin-MLL inhibitor-23 is the enantiomer of Menin-MLL inhibitor-23. | |
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V4201 | (R)-BAY1238097 | 1564269-85-7 | R)-BAY1238097 is the R-isomer of BAY-1238097 with lower activity than BAY1238097. |
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V77361 | (S)-Bleximenib oxalate ((S)-Menin-MLL inhibitor 24 oxalate) | (S)-Bleximenib ((S)-Menin-MLL inhibitor 24) oxalate is the S-enantiomer of (S)-Menin-MLL inhibitor 24 oxalate. | |
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V56124 | (S)-GNE-987 | 2738533-33-8 | (S)-GNE-987 (compound 4), the hydroxyproline epimer of GNE-987 (BET degrader), can eliminate the binding to von Hippel-Lindau and cannot degrade BRD4 protein. |
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V56138 | (S,R)-CFT8634 | 2704617-95-6 | (S,R)-CFT8634 is a selective and orally bioactive BRD9 protein degrader. |
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V52483 | 6-O-Isobutyrylbritannilactone | 1259933-02-2 | 6-O-Isobutyrylbritannilactone is a natural melanogenesis inhibitor. |
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V52488 | 653-47 | 1224678-75-4 | 653-47 is an enhancer that significantly enhances the cAMP response element binding protein (CREB) inhibitory activity of 666-15. |
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V52487 | 653-47 hydrochloride | 1224567-46-7 | 653-47 HCl is an enhancer that significantly enhances the cAMP response element binding protein (CREB) inhibitory activity of 666-15. |
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V5228 | 666-15 | 1433286-70-4 | 666-15 is a novel, cell-permeable, potent and selective inhibitor ofCREB (cAMP-response element binding protein)-mediated gene transcription with IC50 of 81 nM. |
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V81843 | 7-O-Methylaloesinol | 105317-69-9 | 7-O-Methylaloesinol is a pigment analogue. |
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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. |
|
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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V0415 | Apabetalone (RVX-08, RVX-000222) | 1044870-39-4 | Apabetalone (also known as RVX-208, RVX000222) is a novel and potent inhibitor of BET (Bromodomain and Extra-Terminal) bromodomain (BD) with potential anti-inflammatory activity and the potential to be used in the treatment of cardiovascular diseases. |
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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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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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