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 Related Products (66):

Cat. No. Product Name Effect Purity
  • HY-13030
    (+)-JQ-1 Inhibitor 99.90%
    (+)-JQ-1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for the first and second bromodomain (BRD4(1/2)).
  • HY-13803
    EPZ-6438 Inhibitor 99.63%
    EPZ-6438 inhibits the activity of human PRC2-containing wild-type EZH2 with Ki of 2.5±0.5 nM.
  • HY-13470
    GSK126 Inhibitor 99.32%
    GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase activity with IC50 of 9.9 nM.
  • HY-15743
    OTX-015 Inhibitor 99.75%
    OTX-015 is a new potent BRD2/3/4 inhibitor for cell adhesion with IC50 values from 92 to 112 nM.
  • HY-13032
    GSK 525762A Inhibitor 99.85%
    GSK 525762A is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
  • HY-102000B
    IACS-9571 Hydrochloride Inhibitor 99.02%
    IACS-9571 Hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
  • HY-100726
    GNE-272 >98.0%
    GNE-272 is a potent and selective in vivo probe for the bromodomains of CBP/EP300 with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.
  • HY-102000
    IACS-9571 Inhibitor
    IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.
  • HY-50698
    BI 2536 Inhibitor 99.19%
    BI 2536 is a potent and selective inhibitor of Plk1 with IC50 of 0.83 nM, and is also a potent inhibitor of BRD4 with IC50 of 25 nM.
  • HY-13500
    GSK343 Inhibitor 99.58%
    GSK343 is a highly potent, selective, and cell-active EZH2 inhibitor with IC50 of 4 nM.
  • HY-12186
    3-Deazaneplanocin A hydrochloride Inhibitor
    3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
  • HY-15646
    UNC1999 Inhibitor 98.01%
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2 (IC50<10 nM) and EZH1 (IC50=45±3 nM).
  • HY-13235
    I-BET151 Inhibitor 98.77%
    I-BET151 is a BET bromodomain inhibitor, inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
  • HY-11006
    KU-57788 Inhibitor 98.74%
    KU-57788 is a potent and selective inhibitor of DNA-PK, a modest inhibitor of BRD4 and BRDT, with IC50s of 13 nM, 1 μM and 3.5 μM, respectively, and also increases CRISPR/Cas9-mediated editing frequencies.
  • HY-16954
    ARV-825 Inhibitor 99.35%
    ARV-825 is a BRD4 Inhibitor based on PROTAC technology.
  • HY-100015
    Mivebresib Inhibitor 99.28%
    Mivebresib, a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo.
  • HY-100972
    ARV-771 Inhibitor 99.44%
    ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader based on PROTAC technology with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively.
  • HY-10409
    TG-101348 Inhibitor 98.28%
    TG-101348 is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3, and also inhibits BRD4 with IC50 of 340 nM.
  • HY-15826
    SGC-CBP30 Inhibitor 99.19%
    SGC-CBP30 is a potent CREBBP/EP300 bromodomain inhibitor with IC50 of 21-69 and 38 nM for CREBBP and EP300 bromodomains, respectively)
  • HY-16652
    RVX-208 Inhibitor 99.19%
    RVX-208 is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.