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 (224):

Cat. No. Product Name Effect Purity
  • HY-13030
    (+)-JQ-1 Inhibitor 99.90%
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))[1]. (+)-JQ-1 also activates autophagy[2].
  • HY-107455
    A-485 Inhibitor
    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 histone acetyltransferase (HAT), respectively[1].
  • HY-N0005
    Curcumin Inhibitor
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
  • 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-13823
    C646 Inhibitor
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases[1].
  • HY-115867
    GSK852 Inhibitor
    GSK852 is a highly potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor (pIC50 = 7.9).
  • HY-145260
    BRD4/CK2-IN-1 Inhibitor
    BRD4/CK2-IN-1 is the first highly effective dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)[1]
  • HY-141890
    BAZ1A-IN-1 Inhibitor
    BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A[1].
  • HY-119374
    BRM/BRG1 ATP Inhibitor-1 Inhibitor 98.49%
    BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM[1].
  • HY-107425
    MZ 1 Inhibitor
    MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively[1].
  • HY-78695
    JQ-1 (carboxylic acid) Inhibitor 99.49%
    JQ-1 carboxylic acid is a (+)-JQ1 derivative (a BET bromodomain inhibitor). JQ-1 carboxylic acid can be used as a precursor to synthesize PROTACs, which targets BET bromodomains[1].
  • HY-101120
    666-15 Inhibitor 99.74%
    666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model[1][2].
  • HY-16954
    ARV-825 Inhibitor 99.32%
    ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
  • HY-112090
    ABBV-744 Inhibitor 99.97%
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with drug-like properties enable the investigation of its antitumor efficacy and tolerability[1].
  • HY-112588
    dBET6 Inhibitor 99.73%
    dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity.
  • 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[1]. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription[4].
  • HY-100972
    ARV-771 Inhibitor 99.82%
    ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively[1].
  • HY-13235
    I-BET151 Inhibitor
    I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively[1][2].
  • HY-101838
    dBET1 Inhibitor 99.24%
    dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker[1].
  • HY-N2020
    Anacardic Acid Inhibitor
    Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ∼8.5 μM and ∼5 μM, respectively.