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 (47):

Cat. No. Product Name Effect Purity
  • HY-13030
    (+)-JQ-1 Inhibitor
    (+)-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
    EPZ-6438 inhibits the activity of human PRC2-containing wild-type EZH2 with Ki of 2.5±0.5 nM.
  • HY-13470
    GSK126 Inhibitor
    GSK126 is a potent, highly selective inhibitor of EZH2 methyltransferase activity with IC50 of 9.9 nM.
  • HY-15743
    OTX-015 Inhibitor
    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
    GSK 525762A is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
  • HY-50698
    BI 2536 Inhibitor
    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
    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-13235
    I-BET151 Inhibitor
    I-BET151 is a BET bromodomain inhibitor, inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
  • HY-15646
    UNC1999 Inhibitor
    UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2 (IC50<10 nM) and EZH1 (IC50=45±3 nM).
  • HY-11006
    KU-57788 Inhibitor
    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-16652
    RVX-208 Inhibitor
    RVX-208 is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87±10 μM and 0.51±0.041 μM for BD1 and BD2, respectively.
  • HY-15826
    SGC-CBP30 Inhibitor
    SGC-CBP30 is a potent CREBBP/EP300 bromodomain inhibitor with IC50 of 21-69 and 38 nM for CREBBP and EP300 bromodomains, respectively)
  • HY-78695
    JQ-1 carboxylic acid Inhibitor
    (+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis.
  • HY-15555
    EPZ005687 Inhibitor
    EPZ005687 is a potent and selective inhibitor of Epigenetic Reader Domain with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
  • HY-13030A
    (R)-(-)-JQ1 Enantiomer Inhibitor
    (-)-JQ-1 is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (−)-JQ1 has no effect.
  • HY-10409
    TG-101348 Inhibitor
    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-13960
    GSK1324726A Inhibitor
    GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
  • HY-15573
    EI1 Inhibitor
    EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.
  • HY-10410
    TG101209 Inhibitor
    TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations; TG101209 inhibit BRD4 activity with IC50 of 130 nM.