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-100351
    BI-7273
    		Inhibitor 99.83%
    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-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-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
  • HY-19999A
    PF-CBP1 hydrochloride
    		Inhibitor 99.99%
    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-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-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-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-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-129937A
    GNE-987
    		Inhibitor 99.91%
    GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
    GNE-987
  • 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-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-19336
    BAZ2-ICR
    		Inhibitor 99.95%
    BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
    BAZ2-ICR
  • 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-148669A
    Bleximenib oxalate
    		Inhibitor ≥98.0%
    Menin-MLL inhibitor 24 (compound A) oxalate is a menin-mixed-lineage leukemia 1 (menin-MLL) inhibitor, and can be used for the research of cancer.
    Bleximenib oxalate
  • 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-100726
    GNE-272
    		Inhibitor 99.76%
    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-101519
    BETd-260
    		Inhibitor 99.59%
    BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
    BETd-260
  • 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-12518
    OF-1
    		Inhibitor 98.93%
    OF-1 is a potent pan-BRPF bromodomain (BRD) inhibitor, with IC50 values of 270 nM, 1.2 μM for TRIM24 and BRPF1B, respectively.
    OF-1
  • HY-120028
    GNE-207
    		Inhibitor
    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
Cat. No. Product Name / Synonyms Application Reactivity