Epigenetic Reader Domain(表观识别蛋白结构域)
Epigenetic regulators of gene expression and chromatin state include so-called writers, erasers, and readers of chromatin modifications.Well-characterized examples of reader domains include bromodomains typically binding acetyllysine and chromatin organization modifier (chromo), malignant brain tumor (MBT), plant homeodomain (PHD), and Tudor domains generally associating with methyllysine. Research on epigenetic readers has been tremendously influenced by the discovery of selective inhibitors targeting the bromodomain and extraterminal motif (BET) family of acetyl-lysine readers. The human genome encodes 46 proteins containing 61 bromodomains clustered into eight families. Distinct experimental approaches are used to identify the first BET inhibitors, GSK 525762A and (+)-JQ-1.
The Polycomb group (PcG) protein, enhancer of zeste homologue 2 (EZH2), has an essential role in promoting histone H3 lysine 27 trimethylation (H3K27me3) and epigenetic gene silencing. This function of EZH2 is important for cell proliferation and inhibition of cell differentiation, and is implicated in cancer progression. Cyclin-dependent kinases regulate epigenetic gene silencing through phosphorylation of EZH2. In many types of cancers including lymphomas and leukemia, EZH2 is postulated to exert its oncogenic effects via aberrant histone and DNA methylation, causing silencing of tumor suppressor genes.
p300/CBP is not only a transcriptional adaptor but also a histone acetyltransferase.
Products for Epigenetic Reader Domain
- Cat.No. 产品名称 Information
- GC19247 MI-503 MI-503 是一种高效且具有口服生物利用度的 menin-mLL 相互作用的小分子抑制剂。
- GC19246 MI-463 An inhibitor of menin-MLL fusion protein interactions
- GC19210 JQ-1 carboxylic acid A selective inhibitor of BET bromodomains
- GC19200 INCB-057643 A BET family protein inhibitor
- GC19119 dBET1 A hybrid molecule containing (+)-JQ-1 and thalidomide
- GC19098 CeMMEC1 A selective TAF1 bromodomain 2 inhibitor
- GC19038 ARV-825 A BRD4 inhibitor that drives BRD4 degradation
- GC18731 LP99 A selective inhibitor of BRD7/9
- GC18729 MZ1 A PROTAC that drives BRD4 degradation
- GC18508 BAY-299 A potent and selective BRD1 inhibitor
- GC16763 NI-57 A BRPF bromodomain inhibitor
- GC13025 GSK6853 A selective chemical probe for the bromodomain of BRPF1
- GC14103 NSC228155 An EGFR activator and inhibitor of KID-KIX interactions
- GC10382 CPI-637 An inhibitor of CBP/EP300 bromodomains
- GC16726 BI-7273 A potent BRD9 bromodomain inhibitor
- GC16817 BI-9564 A selective BRD9/7 bromodomain inhibitor
- GC12588 I-BRD9 A BRD9 bromodomain inhibitor
- GC15789 GSK2801 A probe for BAZ2A/B bromodomains
- GC10979 PFI 4 A chemical probe for BRPF1
- GC16299 BET bromodomain inhibitor BET 溴结构域抑制剂是从专利 WO/2015/153871A2 化合物实施例 11 中提取的一种有效的 BET 抑制剂。
- GC12440 GSK 5959 An inhibitor of the BRPF1 bromodomain
- GC15175 BAZ2-ICR A BAZ2A/B bromodomain inhibitor
- GC17482 OF-1 A bromodomain probe for BRPF proteins
- GC14361 PFI 3 Probe for bromodomains of SMARCA2/4 and PB1(bromodomain 5)
- GC16599 CPI-169 A selective EZH2 inhibitor
- GC12733 C646 C646是一种有效的选择性p300/CBP组蛋白乙酰转移酶抑制剂(Ki 400 nM),已被证明具有神经保护、抗癌和抗上皮间质转化(anti-EMT)等多种作用。.
- GC14699 CPI-203 A bioavailable inhibitor of BET bromodomains
- GC14063 GSK1324726A A selective inhibitor of BET family proteins
- GC13148 MS436 MS436 是一类新的溴结构域抑制剂,对 BRD4 BrD1 具有估计的 Ki=30-50 nM 的强亲和力,对 BrD2 的选择性是 10 倍。
- GC15747 I-BET151 (GSK1210151A) A BRD2, BRD3, and BRD4 inhibitor
- GC17073 I-BET-762 Inhibitor of BET proteins
- GC11439 MG 149 A HAT inhibitor
- GC14199 RVX-208 A selective BET bromodomain antagonist
- GC12450 BI 2536 A potent inhibitor of Plk1
- GC10174 SGC-CBP30 A potent inhibitor of CREBBP/EP300 bromodomains
- GC12419 UNC 926 hydrochloride An antagonist of L3MBTL1, L3MBTL3, and L3MBTL4
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GC17284
Anacardic acid
A histone acetyltransferase inhibitor
- GC17973 OTX-015 A BRD2, BRD3, and BRD4 inhibitor
- GC12199 MI-3 An inhibitor of menin-MLL fusion protein interactions
- GC11418 MI-2 An inhibitor of menin-MLL fusion protein interactions
- GC14787 Curcumin A yellow pigment with diverse biological activities
- GC10402 Bromosporine A non-specific bromodomain inhibitor
- GC15375 PFI-1 (PF-6405761) A BET bromodomain inhibitor
- GC13822 (-)-JQ1 A selective inhibitor of BET bromodomains
- GC16531 Bromodomain Inhibitor, (+)-JQ1 A selective inhibitor of BET bromodomains