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 (64):

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/33 nM。
  • HY-13803
    EPZ-6438 Inhibitor 99.63%
    EPZ-6438 抑制含人PRC2的野生型EZH2Ki 为 2.5±0.5 nM。
  • HY-13470
    GSK126 Inhibitor 99.32%
    GSK126 是一种有效的选择性EZH2 甲基转移酶抑制剂,IC50 为 9.9 nM。
  • HY-15743
    OTX-015 Inhibitor 99.75%
    OTX-015 是一种有效的 BRD2/3/4 抑制剂,能够抑制细胞增殖,IC50 值为 92-112 nM。
  • HY-13032
    GSK 525762A Inhibitor 99.22%
    GSK 525762A 是一种 BET bromodomain 抑制剂,IC50 为 32.5-42.5 nM。
  • 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-12863
    CPI-0610 99.88%
    CPI-0610是一种有效的选择性 BET溴区抑制剂, 抑制BRD4-BD1, IC50值为39 nM。
  • HY-102000B
    IACS-9571 Hydrochloride Inhibitor 99.02%
    IACS-9571 Hydrochloride 是溴结构域蛋白 TRIM24BRPF1 的抑制剂,对 TRIM24 的 IC50Kd 值分别为 8 nM 和 31 nM,对 BRPF1 的 Kd 值为 14 nM。
  • HY-50698
    BI 2536 Inhibitor 99.19%
    BI 2536 是一种有效的选择性的 Plk1 抑制剂,IC50 为 0.83 nM,也有效抑制 BRD4IC50 为 25 nM。
  • HY-13500
    GSK343 Inhibitor 99.58%
    GSK343 是一种高效的选择性EZH2 抑制剂,IC50 为 4 nM。
  • HY-12186
    3-Deazaneplanocin A hydrochloride Inhibitor
    3-Deazaneplanocin A hydrochloride 是一种有效的组蛋白甲基转移酶 (EZH2) 抑制剂。
  • HY-15646
    UNC1999 Inhibitor 99.02%
    UNC1999 是一种有效的 SAM- 竞争性的选择性 EZH2EZH1 抑制剂,IC50 分别为 <10 nM 和 45±3 nM。
  • HY-13235
    I-BET151 Inhibitor 98.77%
    I-BET151 是一种 BET溴区 (BET bromodomain) 抑制剂,抑制 BRD4BRD2BRD3pIC50 分别为 6.1,6.3 和 6.6。
  • HY-11006
    KU-57788 Inhibitor 98.74%
    KU-57788 是一种有效的,选择性的 DNA-PK 抑制剂,并且适度抑制 BRD4BRDTIC50 值分别为 13 nM,1 μM 和 3.5 μM;同时能够激活 CRISPR/Cas9
  • HY-16954
    ARV-825 Inhibitor 99.35%
    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,Kds 值分别为 90 和 28 nM
  • HY-100015
    Mivebresib Inhibitor 99.28%
    Mivebresib是BET家族的抑制剂,能够扰乱关键的转录程序在体内或者体外推动前列腺癌增长引起强的抗肿瘤特性,也是MYC和TMPRSS2-ETS的抑制剂。
  • HY-15826
    SGC-CBP30 Inhibitor 99.19%
    SGC-CBP30是CREBBP和EP300的布罗莫结构域抑制剂,IC50分别为21-69nM和38 nM。
  • HY-16652
    RVX-208 Inhibitor 99.19%
    RVX-208 是一种 BET 转录抑制剂,作用于 BD1BD2IC50 分别为 87±10 μM 和 0.51±0.041 μM。
  • HY-13030A
    (R)-(-)-JQ1 Enantiomer Inhibitor 99.61%
    (-)-JQ-1 是 (+)-JQ1的异构体。(+)-JQ1有效 降低 BRD4 基因表达,而s (−)-JQ1 没有此作用效果。
  • HY-100972
    ARV-771 Inhibitor 99.44%
    ARV-771 是 PROTAC 类的有效 BET 降解剂。对 BRD2, BRD3 和 BRD4 的 Kd 值分别为 4.7, 7.6 和 7.6 nM。