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 (100):

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-13470
    GSK126 Inhibitor 99.86%
    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-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-15743
    OTX-015 Inhibitor 99.81%
    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-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-112090
    ABBV-744 Inhibitor
    ABBV-744 是一种结合域 II 选择性的 BET bromodomain 抑制剂,可用于炎症,癌症,艾滋病等的研究。
  • HY-111422
    PLX51107 Inhibitor 99.81%
    PLX51107 是一种有效的,选择性的 BET 抑制剂,对 BRD2,BRD3,BRD4 和 BRDT 的 BD1 结构域的亲和力 Kd 值分别为 1.6,2.1,1.7 和 5 nM,BD2 结构域亲和力 Kd 值分别为 5.9,6.2,6.1 和 120 nM;PLX51107 同时与 CBP 和 EP300 的结构域相互作用 (Kd,∼ 100 nM)。
  • HY-103299
    KG-501 Inhibitor 99.12%
    KG-501 是 CREB 的抑制剂,其 IC50 值为 6.89 μM。
  • HY-N0005
    Curcumin Inhibitor 99.66%
    Curcumin 是一种天然的酚类化合物,具有显著的抗氧化作用,通过激活 Nrf2 来起到化疗作用,同时为与 p300/CREB 结合的组蛋白乙酰转移酶 (histone acetyltransferase) 的抑制剂。
  • HY-13032
    GSK 525762A Inhibitor 99.85%
    GSK 525762A 是一种 BET bromodomain 抑制剂,IC50 为 32.5-42.5 nM。
  • 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,Kd 值分别为 90 和 28 nM。
  • 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。
  • HY-13500
    GSK343 Inhibitor 98.49%
    GSK343 是一种高效的选择性EZH2 抑制剂,IC50 为 4 nM。
  • HY-50698
    BI 2536 Inhibitor 99.95%
    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-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溴区 (BET bromodomain) 抑制剂,抑制 BRD4BRD2BRD3pIC50 分别为 6.1,6.3 和 6.6。
  • HY-100015
    Mivebresib Inhibitor 99.28%
  • HY-15646
    UNC1999 Inhibitor 99.47%
    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-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-78695
    JQ-1 carboxylic acid Inhibitor 99.59%
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