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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V77101 | DC-BPi-11 hydrochloride | DC-BPi-11 HCl is an inhibitor (blocker/antagonist) of bromodomain PHD finger transcription factor (BPTF) with IC50 of 698 nM. | |
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V79857 | DDO-8926 | DDO-8926 is a potent and specific BET inhibitor that can significantly reduce mechanical hypersensitivity by inhibiting the expression of pro-inflammatory cytokines and reducing excitability, and may be used in neuropathic pain research. | |
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V85242 | DW71177 | 2241311-72-6 | |
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V2694 | EED226 | 2083627-02-3 | EED226 (EED-226) is a first-in-class, selective, orally bioavailable and allosteric inhibitor of embryonic ectoderm development (EED) with potential anticancer activity. |
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V34753 | Eleven-Nineteen-Leukemia Protein IN-1 | 2894121-68-5 | Eleven-Nineteen-Leukemia Protein IN-1 is an inhibitor (blocker/antagonist) of the ENL YEATS domain with IC50 of 14.5 nM. |
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V34754 | Eleven-Nineteen-Leukemia Protein IN-2 | 2894121-78-7 | Eleven-Nineteen-Leukemia Protein IN-2 (compound 23) is an Eleven-Nineteen-Leukemia Protein (ENL) inhibitor (antagonist) with IC50 of 10.7 nM. |
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V34752 | Eleven-Nineteen-Leukemia Protein IN-3 | 2894121-83-4 | Eleven-Nineteen-Leukemia Protein IN-3 is an orally bioactive ENL YEATS domain inhibitor (antagonist) with IC50 of 15.4 nM. |
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V56128 | Emilumenib (Menin-MLL inhibitor 26) | 2440018-29-9 | Emilumenib (Menin-MLL inhibitor 26) is a Menin-MLL inhibitor. |
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V84615 | EP300/CBP-IN-1 | 2638507-71-6 | |
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V84907 | EP300/CBP-IN-2 | 2379527-49-6 | |
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V51412 | FHD-609 | 2676211-64-4 | FHD-609 is a modification and modifier of the Brownian domain-containing protein BRD9. |
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V85305 | FHT-2344 | 2468058-90-2 | |
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V31685 | FL-411 | 2118944-88-8 | FL-411 is a potent and specific BRD4 inhibitor that can suppress BRD4(1) with IC50 of 0.43±0.09 μM. |
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V4552 | GNE-272 | 1936428-93-1 | GNE-272 is a novel, potent and selectivein vivochemical probe for and inhibitor of the CBP/EP300bromodomainswithIC50values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. |
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V4553 | GNE-781 | 1936422-33-1 | GNE-781 (GNE781) is a novel, highly potent and selectiveinhibitor of CBP (Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein) with immunomodulatory and anticancer effects. |
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V56146 | GNE-886 | 2101957-05-3 | GNE-886 (Compound 21) is a potent and specific inhibitor of cat eye syndrome chromosome candidate region 2 bromodomain (CECR2, BRD) with IC50 of 0.016 µM and EC50 of 370 nM. |
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V4084 | GSK-5959 | 901245-65-6 | GSK5959 is a novel, potent, selective and cell permeableBRPF1 (bromodomain and PHD finger-containing) bromodomaininhibitor with an IC50 of 80 nM. |
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V79657 | GSK023 | GSK023 (compound 31) is a selective chemical probe targeting the BD1 domain of BET. | |
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V56126 | GSK040 | 2752331-09-0 | GSK040 is a potent and specific BET BD2 inhibitor (antagonist) with pIC50 of 8.3. |
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V52039 | GSK097 | 2159137-02-5 | GSK097 is a potent and specific inhibitor of bromoalkanes and BET protein second bromoalkane (BD2). |
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