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 |
|---|---|---|---|---|
|
V84947 | BET-IN-23 | 2953287-57-3 | |
|
V84336 | BET-IN-24 | 2407658-21-1 | |
|
V75495 | BET-IN-6 | 2570470-39-0 | BET-IN-6 is a potent and high-affinity BRD2/BRD4 inhibitor. |
|
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. |
|
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. |
|
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. |
|
V8789 | BI-894999 | 1660117-38-3 | BI-894999 is a novel, and selective BET inhibitor that has the potential to be used for the treatment of hematological malignancies by repression of super-enhancer driven oncogenes. |
|
V2909 | BI-9564 | 1883429-22-8 | BI-9564 is a novel, cell-permeable, noncytotoxic, potent, and selective inhibitor of BRD9 (bromodomain-containing protein) and BRD7 BD (bromodomains) with Kd values of 14.1 and 239 nM, and IC50 values of 75 nM and 3.4 µM for BRD9/7 respectively. |
|
V78414 | BI01826025 (pArg-JQ1) | BI01826025 (pArg-JQ1) is a BRDT bromodomain1 (BRDTBD1) PROTAC degrader. | |
|
V34755 | Biotinylated-JQ1 (Biotin-JQ1) | 1635437-52-3 | Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated analogue of JQ1 that binds to the BRD4 bromodomain with high affinity. |
|
V0425 | Birabresib (OTX015; MK8628) | 202590-98-5 | Birabresib (formerly OTX-015; MK-8628) is a potent and orally bioavailable inhibitor of BET bromodomain (BRD2/3/4) with antineoplastic activity. |
|
V56121 | Bleximenib (Menin-MLL inhibitor 24) | 2654081-35-1 | Bleximenib (Menin-MLL inhibitor 24) is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor. |
|
V56119 | Bleximenib oxalate (Menin-MLL inhibitor 24 oxalate) | 2866179-95-3 | Bleximenib (Menin-MLL inhibitor 24) oxalate is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor for cancer research. |
|
V3467 | BMS-986158 | 1800340-40-2 | BMS-986158 (BMS986158; BMS 986158) is a novel, potent and selective BET (bromodomain and extra-terminal) protein inhibitor with potential antineoplastic activity. |
|
V75500 | BN-104 (BNM-1192; Menin-MLL inhibitor 27) | 2938995-50-5 | Menin-MLL inhibitor 27 can inhibit Menin-MLL interaction and may be utilized in cancer-related research, like acute myeloid leukemia. |
|
V52895 | BPTF-IN-BZ1 | 2766623-38-3 | BPTF-IN-BZ1 is a BPTF inhibitor (antagonist) with high potency (Kd = 6.3 nM). |
|
V75496 | BRD4 D1-IN-1 | 2863623-98-5 | BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). |
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V75501 | BRD4 D1-IN-2 | 2863687-22-1 | BRD4 D1-IN-2 (compound 26) is a potent and specific BRD4 D1 inhibitor (IC50<0.092 µM). |
|
V75502 | BRD4 Inhibitor-17 | 2835555-10-5 | BRD4 Inhibitor-17 (Compound 5i) is a potent BRD4 inhibitor (antagonist) with IC50 of 0.33 μM. |
|
V78477 | BRD4 Inhibitor-25 | BRD4 Inhibitor-25 is a BRD4 inhibitor (antagonist) with IC50 of 0.82 μM and 1.94 μM for the BD1 and BD2 domains of BRD4. |
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