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 (107):

Cat. No. Product Name Effect Purity
  • HY-13030
    (+)-JQ-1 Inhibitor 99.90%
    (+)-JQ-1 is a BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)).
  • HY-13470
    GSK126 Inhibitor 99.86%
    GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.
  • HY-15743
    Birabresib Inhibitor 99.81%
    Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.
  • HY-107455
    A-485 Inhibitor 99.08%
    A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP, respectively.
  • HY-N0005
    Curcumin Inhibitor 99.66%
    Curcumin is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase ((HATs)) and also shows inhibitory effects on NF-κB and MAPKs.
  • HY-103299
    KG-501 Inhibitor 99.12%
    KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.
  • HY-108696
    GNE-781 Inhibitor
    GNE-781 is a highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nΜ, respectively.
  • HY-111519
    dTRIM24 Inhibitor 98.20%
    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
  • 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-16954
    ARV-825 Inhibitor 99.37%
    ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
  • HY-50698
    BI 2536 Inhibitor 99.95%
    BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively.
  • HY-13500
    GSK343 Inhibitor 98.49%
    GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
  • HY-13823
    C646 Inhibitor >98.0%
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
  • HY-13235
    I-BET151 Inhibitor 98.77%
    I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
  • HY-12186
    3-Deazaneplanocin A hydrochloride Inhibitor 99.76%
    3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
  • HY-101120
    666-15 Inhibitor 98.65%
    666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.
  • HY-100482
    CPI-637 Inhibitor 99.94%
    CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.
  • HY-15646
    UNC1999 Inhibitor 99.47%
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH1/2 with IC50s of 10 nM and 45 nM, repectively.
  • HY-100015
    Mivebresib Inhibitor 99.28%
    Mivebresib is a potent and orally available bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
  • HY-101838
    dBET1 Inhibitor 99.24%
    dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
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