2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain

Epigenetic Reader Domain

Epigenetic Reader Domain

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-119374
    BRM/BRG1 ATP Inhibitor-1
    		Inhibitor 99.72%
    BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active 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. BRM/BRG1 ATP Inhibitor-1 has anticancer activity.
    BRM/BRG1 ATP Inhibitor-1
  • HY-15887
    MG 149
    		Inhibitor 99.60%
    MG149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50 = 47 uM); little potent for PCAF and p300 (IC50 >200 uM). MG 149 inhibits KAT8 and blocks PINK1 kinase activity. MG149 inhibits the phosphorylation of Parkin and ubiquitin, thereby suppressing the initiation of PINK1-dependent mitophagy. MG 149 can reverse chronic restraint stress (CRS) induced hypertension and related molecular changes. MG 149 commonly used in research on diseases such as hypertension and Parkinson's disease.
    MG 149
  • HY-100972
    ARV-771
    		Degrader 99.87%
    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.
    ARV-771
  • 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.
    dBET1
  • HY-132001
    Ziftomenib
    		Inhibitor 99.43%
    Ziftomenib (KO-539) is an orally active menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).
    Ziftomenib
  • HY-N2020
    Anacardic Acid
    		Inhibitor 98.49%
    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.
    Anacardic Acid
  • HY-13235
    I-BET151
    		Inhibitor 99.47%
    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.
    I-BET151
  • HY-78695
    JQ-1 carboxylic acid
    		Inhibitor 99.69%
    JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
    JQ-1 carboxylic acid
  • HY-101084
    NSC 228155
    		Inhibitor
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
    NSC 228155
  • HY-103299
    KG-501
    		Inhibitor 99.45%
    KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.
    KG-501
  • HY-153367
    FHD-609
    		Inhibitor 98.95%
    FHD-609 is a PROTAC degrader and inhibitor of BRD9 (Bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment. (Blue: BRD9 ligand-6 (HY-49393), Black: linker (HY-168309); Pink: (S)-Deoxy-thalidomide-Br (HY-168308) ).
    FHD-609
  • HY-12863
    Pelabresib
    		Inhibitor 99.95%
    Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.
    Pelabresib
  • HY-13032
    Molibresib
    		Inhibitor 99.94%
    Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
    Molibresib
  • 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 agent-like properties enable the investigation of its antitumor efficacy and tolerability.
    ABBV-744
  • HY-134582
    dCBP-1
    		Inhibitor 99.37%
    dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
    dCBP-1
  • HY-12583
    A-366
    		Inhibitor 98.13%
    A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
    A-366
  • HY-163410
    AU-24118
    		Degrader 99.10%
    AU-24118 is a selective and orally bioavailable PROTAC degrader of mSWI-SNF ATPases (SMARCA2 and SMARCA4) and PBRM1. AU-24118 integrates a bait moiety binding to the bromodomains of SMARCA2 and SMARCA4, along with a ligand moiety for CRBN ligase. AU-24118 demonstrates tumor regression in prostate cancer model. AU-24118 can be studied to combat prostate cancer. (Pink: PBRM1/SMARCA2,4 ligand (HY-171774); Blue: CRBN ligand (HY-171775)).
    AU-24118
  • HY-151923
    ATF3 inducer 1
    		Inhibitor 99.61%
    ATF3 inducer 1 is a potent ATF3 inducer. ATF3 inducer 1 increases the ATF3 protein and ATF3 mRNA expression. ATF3 inducer 1 shows anti-MetS activity in mouse.
    ATF3 inducer 1
  • HY-100351
    BI-7273
    		Inhibitor 99.75%
    BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.
    BI-7273
  • HY-100015
    Mivebresib
    		Inhibitor 99.29%
    Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.
    Mivebresib
Cat. No. Product Name / Synonyms Application Reactivity