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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V2515 | Menin-MLL inhibitor 20 | 2448173-47-3 | Menin-MLL inhibitor 20 is an irreversible inhibitor of the menin-MLL interaction and has anti-tumor activity (WO2020142557A1, Intermediate 6). |
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V80740 | Menin-MLL inhibitor 29 | Menin-MLL inhibitor 29 (Compound C1) is a Menin-MLL PPI inhibitor. | |
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V32467 | MI-136 | 1628316-74-4 | MI-136 is an inhibitor (blocker/antagonist) of menin-MLL (PPI) protein interaction with IC50 of 31 nM and Kd of 23.6 nM. |
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V0396 | MI-2 (Menin-MLL Inhibitor) | 1271738-62-5 | MI-2 (MI2, Menin-MLL Inhibitor) is a novel, potent and selectiveinhibitor of menin-MLL interaction with antineoplastic activity. |
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V2601 | MI-463 | 1628317-18-9 | MI-463 is a novel potent & orally bioactive inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM. |
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V2964 | Mivebresib | 1445993-26-9 | Mivebresib (formerly known as ABBV-075) is a novel potent bromodomain (BRD) inhibitor that is being tested in a Phase I study for the treatment of solid tumors. |
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V0414 | Molibresib (I-BET762; GSK-525762A) | 1260907-17-2 | Molibresib (also known as GSK525762A,I-BET-762, GSK-525762)is a novel and potent inhibitor for BET (Bromodomain and Extra-Terminal) family of proteins with potential anti-inflammatory and anticancer activity. |
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V32069 | Molibresib besylate | 1895049-20-3 | Molibresib besylate(GSK-525762C; I-BET-762 besylate) is a novel and potent BET bromodomain inhibitor with IC50 of 32.5-42.5 nM and has immunomodulatory activity. |
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V41163 | MS31 | 2366264-12-0 | MS31 is a high-affinity, selective, fragment-like inhibitor of the methyl lysine reading and writing protein spindlin 1 (SPIN1), which effectively disrupts the interaction between SPIN1 and H3K4me3 proteins (IC50=77 nM, AlphaLISA; 243 nM , FP). |
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V0421 | MS436 | 1395084-25-9 | MS436 (MS-346), a diazobenzene analog,is a novel, potent and selective inhibitor of BET/BRD4bromodomain with potential anti-inflammatory activity. |
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V41121 | NEO2734 (EP31670) | 2081072-29-7 | NEO2734 (EP31670) is an orally bioactive, selective inhibitor of p300/CBP and BET bromodomain with IC50s <30 nM. |
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V26460 | NI-57 | 1883548-89-7 | NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively |
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V82337 | Nrf2 activator-2 | 2770448-53-6 | Nrf2 activator-2 (compound O15) is an osthole analogue and a potent Nrf2 agonist/activator with EC50 of 2.9 μM in 293 T cells. |
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V56123 | NVS-BET-1 | 1639115-52-8 | NVS-BET-1 is a BET bromodomain inhibitor that regulates keratinocyte plasticity. |
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V41075 | OARV-771 | 2683008-37-7 | OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. |
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V0420 | OF-1 (OF-1) | 919973-83-4 | OF-1 (OF1; SGC-OF-1) is a potent and selective inhibitor of bromodomain and PHD finger containing protein 1 (BRPF1)with important biological activity. |
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V41036 | PBRM1-BD2-IN-1 | 1915012-21-3 | PBRM1-BD2-IN-1 is a selective and cellularly active PBRM1 bromodomain inhibitor. |
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V41035 | PBRM1-BD2-IN-2 | 2819989-57-4 | PBRM1-BD2-IN-2 is a selective and cellularly active PBRM1 bromodomain inhibitor. |
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V56151 | PBRM1-BD2-IN-3 | 2819989-58-5 | PBRM1-BD2-IN-3 (compound 12) is a potent inhibitor of PBRM1-BD2 with IC50 of 1.1 μM. |
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V56142 | PBRM1-BD2-IN-4 | 2819989-60-9 | PBRM1-BD2-IN-4 (compound 15) is a potent PBRM1 bromodomain inhibitor (antagonist) with Kd of 5.5 μM and 11.1 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and IC50 of 0.2 μM for PBRM1-BD2. |
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