1. Epigenetics
  2. Epigenetic Reader Domain

Epigenetic Reader Domain

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.

Epigenetic Reader Domain 相关产品 (103):

Cat. No. Product Name Effect Purity
  • HY-13030
    (+)-JQ-1 Inhibitor 99.90%
    (+)-JQ-1 是一种 BET bromodomain 抑制剂,抑制 BRD4(1/2)IC50 分别为 77 nM 和 33 nM。
  • HY-13470
    GSK126 Inhibitor 99.86%
    GSK126 是一种有效,选择性的 EZH2 甲基转移酶抑制剂,IC50 为 9.9 nM。
  • HY-13803
    EPZ-6438 Inhibitor 99.63%
    EPZ-6438 (Tazemetostat)是一种有效,选择性,口服的 EZH2 抑制剂,KiIC50 分别为2.5和11 nM。
  • HY-15743
    OTX-015 Inhibitor 99.81%
    OTX-015 是一种有效的 BRD2/3/4 抑制剂,IC50 值为 92-112 nM。
  • HY-107455
    A-485 Inhibitor 99.08%
    A-485 是 p300/CBP 的强效选择性催化抑制剂,对 p300CBPIC50 值分别为 9.8 nM 和 2.6 nM。
  • HY-112588
    dBET6 Inhibitor 99.40%
    dBET6 是一种高效的,选择性的,细胞透过的 BET 降解剂,IC50 值为 14 nM,具有抗肿瘤活性。
  • HY-103299
    KG-501 Inhibitor 99.12%
    KG-501 是 CREB 的抑制剂,其 IC50 值为 6.89 μM。
  • HY-101519
    BETd-260 Inhibitor 98.04%
    BETd-260 是基于 PROTAC 技术的一种有效的 BET 降解剂,在白血病细胞 RS4;11 中,降低 BRD4 蛋白活性,IC50 值为 30 pM。
  • HY-N0005
    Curcumin Inhibitor 99.66%
    Curcumin是一种天然酚类化合物,具有抗炎,抗氧化,抗增殖和抗血管生成等多种活性。 Curcumin是p300组蛋白乙酰转移酶 ((HATs)) 抑制剂,也显示对 NF-κBMAPKs 的抑制作用。
  • HY-100972
    ARV-771 Inhibitor 99.44%
    ARV-771 是 PROTAC 类的有效的 BET 降解剂。对 BRD2, BRD3 和 BRD4 的 Kd 值分别为 4.7, 7.6 和 7.6 nM。
  • HY-16954
    ARV-825 Inhibitor 99.37%
    ARV-825 是一种 PROTAC 类的 BRD4 抑制剂。ARV-825 对 BRD4 的 BD1 和 BD2 结构域具有高亲和力,Kd 值分别为 90 和 28 nM。
  • HY-13032
    GSK 525762A Inhibitor 99.85%
    GSK 525762A是 BET 溴结构域 抑制剂,IC50 为32.5-42.5 nM。
  • HY-50698
    BI 2536 Inhibitor 99.95%
    BI 2536是 PLK1BRD4 的双抑制剂,IC50 分别为0.83 和 25 nM。
  • HY-13500
    GSK343 Inhibitor 98.49%
    GSK343 是一种高效,选择性的 EZH2 抑制剂,IC50 为 4 nM。
  • HY-12186
    3-Deazaneplanocin A hydrochloride Inhibitor 99.76%
    3-Deazaneplanocin A hydrochloride 是一种有效的组蛋白甲基转移酶 (EZH2) 抑制剂。
  • HY-13235
    I-BET151 Inhibitor 98.77%
    I-BET151 是一种 BET溴结构域 (BET bromodomain) 抑制剂,抑制 BRD4BRD2BRD3pIC50 分别为 6.1,6.3 和 6.6。
  • HY-13823
    C646 Inhibitor >98.0%
    C646 是选择性,竞争性的 histone acetyltransferase p300 抑制剂,Ki 值为 400 nM,对其他的乙酰转移酶作用较小。
  • HY-101120
    666-15 Inhibitor 98.65%
    666-15是有效选择性的CREB抑制剂,IC50值为81 nM。
  • HY-15646
    UNC1999 Inhibitor 99.47%
    UNC1999 是一种有效,选择性和SAM-竞争性的 EZH2EZH1 抑制剂,IC50 分别为 10 nM 和 45 nM。
  • HY-100482
    CPI-637 Inhibitor 99.94%
    CPI-637是一个强的和有选择性的CBP/EP300 bromodomains的抑制剂,在CBP/EP300 和 BRD4中的IC50分别是 0.03±0.01μM 和 11.0±0.6 μM。
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