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-145446
    SGC-SMARCA-BRDVIII
    		Inhibitor 99.92%
    SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2/4 and PB1(5), with Kds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII also inhibits PB1(2) and PB1(3), with Kds of 3.7 and 2.0 μM, respectively. SGC-SMARCA-BRDVIII can block adipogenesis of 3T3-L1 murine fibroblasts.
    SGC-SMARCA-BRDVIII
  • HY-137573
    Trotabresib
    		Inhibitor 99.53%
    CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors.
    Trotabresib
  • HY-100726
    GNE-272
    		Inhibitor 99.60%
    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.
    GNE-272
  • HY-19541
    I-CBP112
    		Inhibitor 98.20%
    I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
    I-CBP112
  • HY-112789
    (+)-JQ1 PA
    		Inhibitor 98.45%
    (+)-JQ1 PA is a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, with an IC50 of 10.4 nM. (+)-JQ1 PA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (+)-JQ1 PA
  • HY-137892
    GSK620
    		Inhibitor 99.79%
    GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
    GSK620
  • HY-19999A
    PF-CBP1 hydrochloride
    		Inhibitor 99.96%
    PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with?IC50?of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β,?IL-6?and?IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates?RGS4?expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.
    PF-CBP1 hydrochloride
  • HY-19809
    MI-463
    		Inhibitor 99.66%
    MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
    MI-463
  • HY-15846
    CPI-203
    		Inhibitor 98.98%
    CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).
    CPI-203
  • HY-149026
    GNE-064
    		Inhibitor 99.65%
    GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of SMARCA4, SMARCA2 and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC50 of 0.035 μM and inhibits SMARCA2 with an EC50 of 0.10 μM. GNE-064 possess Kds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis.
    GNE-064
  • HY-117690
    dBRD9
    		Degrader 99.89%
    dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family.
    dBRD9
  • HY-136521
    AZ13824374
    		Inhibitor 98.86%
    AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. AZ13824374 inhibits ATAD2 with pIC50s of 8.2 and 6.2 in ATAD2 FRET assay and ATAD2 NanoBRET assay, respectively.
    AZ13824374
  • HY-120028
    GNE-207
    		Inhibitor 99.94%
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
    GNE-207
  • HY-129939
    PROTAC BRD4 ligand-1
    		Inhibitor 99.85%
    PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A).
    PROTAC BRD4 ligand-1
  • HY-100352
    BI-9564
    		Inhibitor 98.73%
    BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family.
    BI-9564
  • HY-16586
    PFI-1
    		Inhibitor 99.87%
    PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.
    PFI-1
  • HY-111139
    MS417
    		Inhibitor 99.79%
    MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
    MS417
  • HY-100653
    AZD5153
    		Inhibitor 99.20%
    AZD5153 (Compound 13) is a trivalent triazolpyrazine bromide domain (BRD), bromodomain and extraterminal (BET) inhibitor. AZD5153 has down-regulated c-Myc gene and tumor growth inhibition activity. AZD5153 can be used in the study of BET small molecule inhibitors .
    AZD5153
  • HY-134463
    NHWD-870
    		Inhibitor 99.36%
    NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.
    NHWD-870
  • HY-13960
    GSK1324726A
    		Inhibitor 99.75%
    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).
    GSK1324726A
Cat. No. Product Name / Synonyms Application Reactivity