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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V79029 | DBr-1 | DBr-1 is a potent BRD9 degrader. | |
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V84538 | dBRD 9-A | 2170679-42-0 | |
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V52198 | dBRD4-BD1 | 2839318-19-1 | dBRD4-BD1 is a selective and persistent BRD4 degrader with DC50 of 280 nM (Dmax=77%). |
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V56122 | DC-BPi-03 | 2758411-46-8 | DC-BPi-03 is a potent BPTF-BRD inhibitor (antagonist) with IC50 of 698.3 nM and Kd of 2.81 μM. |
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V52196 | DC-BPi-11 | 2758411-61-7 | DC-BPi-11 is an inhibitor (blocker/antagonist) of bromodomain PHD finger transcription factor (BPTF) with IC50 of 698 nM. |
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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. | |
|
V100317 | DCSM06 | 924855-67-4 | DCSM06 is a bromodomain inhibitor of the SWI/SNF chromatin remodeling complex SMARCA2 with IC50 of 9.7 μM. |
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V100259 | DCSM06-05 | 880811-10-9 | DCSM06-05 is a potent SMARCA2-BRD inhibitor with IC50 of 9 µM and Kd of 22.4 µM. |
|
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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V88854 | DN02 | DN02 is a potent and selective BRD8 bromodomain probe. | |
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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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V56128 | Emilumenib (Menin-MLL inhibitor 26) | 2440018-29-9 | Emilumenib (Menin-MLL inhibitor 26) is a Menin-MLL inhibitor. |
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V98455 | EP300/CBP ligand 2 | EP300/CBP ligand 2 (compound S19) is a ligand that targets the bromodomains of CREB-binding protein (CBP) and E1A-associated protein (EP300). | |
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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. |
|
V85305 | FHT-2344 | 2468058-90-2 | |
|
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. |
|
V103576 | Gal-ARV-771 | Gal-ARV-771 is a PROTAC prodrug that is ARV-771 modified with galactose. |
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