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.

Epigenetic Reader Domain Isoform Specific Products:

Epigenetic Reader Domain Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-161889
    DCSM06-05
    		Inhibitor
    DCSM06-05 is a potent SMARCA2-BRD inhibitor with an IC50 value of 9 µM, a Kd value of 22.4 µM.
    DCSM06-05
  • HY-114207
    VinSpinIn
    		Inhibitor
    VinSpinIn is a Spindlin1 inhibitor (KD: 9.9 nM for SPIN149-262). VinSpinIn is a chemical probe for tudor domain of Spindlin1. VinSpinIn can be used to study chromatin function.
    VinSpinIn
  • HY-104072
    BRD4-IN-3
    		Inhibitor
    BRD4-IN-3 (compound 141) is a potent BRD4 inhibitor with an IC50 of <0.5 µM. BRD4-IN-3 shows cytoxicity for MYC-Raji with an IC50 value of >1 µM.
    BRD4-IN-3
  • HY-153593
    BET bromodomain inhibitor 3
    		Inhibitor
    BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with Ki value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease.
    BET bromodomain inhibitor 3
  • HY-W494890
    SMARCA2-IN-10
    		Inhibitor
    SMARCA2-IN-10 (Compound 4) is a highly selective SMARCA2 ATPase domain inhibitor (IC50=17.676 μM). SMARCA2-IN-10 induces cell death in SMARCA4-deficient tumors. SMARCA2-IN-10 is promising for research of SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma.
    SMARCA2-IN-10
  • HY-161884
    SMARCA2/4-IN-1
    		Inhibitor
    SMARCA2/4-IN-1 (compound 1) is a potent SMARCA2 inhibitor with IC50 values of 3.8, 1.7 µM for SMARCA2, SMARCA4, respectively.
    SMARCA2/4-IN-1
  • HY-115663
    C620-0696
    		Inhibitor
    C620-0696 is an inhibitor targeting the brom domain of BPTF, with a KD value of 35.5 μM. C620-0696 can exert cytotoxic effects on A549 and H358 cells, inhibiting the expression of c-Myc. C620-0696 inhibits cell migration and colony formation, and induces apoptosis and cell cycle arrest. C620-0696 can be used in the research of non-small cell lung cancer.
    C620-0696
  • HY-152469
    Eleven-Nineteen-Leukemia Protein IN-1
    		Inhibitor
    Eleven-Nineteen-Leukemia Protein IN-1 is an inhibitor of ENL YEATS domain with an IC50 value of 14.5 nM. Eleven-Nineteen-Leukemia Protein IN-1 interacts with ENL protein and enhances the thermal stability of ENL protein in vitro.
    Eleven-Nineteen-Leukemia Protein IN-1
  • HY-163108
    ATAD2-IN-1
    		Inhibitor
    ATAD2-IN-1 (compound 19f) is a potent ATAD2 inhibitor (IC50: 0.27 μM) and can induce apoptosis. ATAD2-IN-1 also inhibits c-Myc activation and BT-549 cell migration.
    ATAD2-IN-1
  • HY-151531
    PBRM1-BD2-IN-4
    		Inhibitor
    PBRM1-BD2-IN-4 is a PBRM1-BD2 inhibitor with an IC50 of 0.2 μM, and its Kd values for PBRM1-BD2 and PBRM1-BD5 are 5.5 μM and 11.1 μM, respectively. PBRM1-BD2-IN-4 selectively inhibits the proliferation of PBRM1-dependent prostate cancer cells. PBRM1-BD2-IN-4 can be used in studies related to prostate cancer.
    PBRM1-BD2-IN-4
  • HY-169487
    SMARCA2 ligand-12
    		Inhibitor
    SMARCA2 ligand-12 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMARCA2 ligand-12 can be used for synthesis PROTAC SMARCA2 degrader-25 (HY-169276).
    SMARCA2 ligand-12
  • HY-W192171
    BRD4 Inhibitor-34
    		Inhibitor
    BRD4 Inhibitor-34 (Compound 12a) is a BRD4 inhibitor with an IC50 of 24 μM.
    BRD4 Inhibitor-34
  • HY-122645
    SMARCA2-IN-4
    		Inhibitor
    SMARCA2-IN-4 (Compound 26) is an inhibitor for SWI/SNF chromatin remodeling complexe SMARCA by targeting the bromodomains. SMARCA2-IN-4 exhibits high affinity for PB1(5), SMARCA2B and SMARCA4 with Kd of 124, 262 and 417 nM.
    SMARCA2-IN-4
  • HY-183247
    BRDT-IN-1
    		Inhibitor
    BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC50 19 nM, Ki 8.8 nM, Ka 1.6 nM, and BRDT-T IC50 56 nM, Ka 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma.
    BRDT-IN-1
  • HY-161495
    CBP/p300 ligand 4
    		Inhibitor
    CBP/p300 ligand 4 (Compound 4) is an orally active inhibitor for CBP/p300 bromodomain, with IC50 of 91.4 nM. CBP/p300 ligand 4 serves as a ligand for target protein XYD190 (HY-161495). XYD190 is a PROTAC degrader for CBP/p300.
    CBP/p300 ligand 4
  • HY-115727
    BET-IN-1
    		Inhibitor
    BET-IN-1 is a potent BET inhibitor that has excellent brain penetration and reasonable metabolic stability.
    BET-IN-1
  • HY-160670
    BRD4-IN-6
    		Inhibitor
    BRD4-IN-6 (compound 116) is a BRD4 inhibitor (extracted from patent CN107721975A).
    BRD4-IN-6
  • HY-180831
    BRD4 D1-IN-3
    		Inhibitor
    BRD4 D1-IN-3 (compound 39) is a potent, selective, and cell-active BRD4-D1 inhibitor (IC50 = 39 nM, Ki = 2.4 nM) with >1700-fold selectivity over BRD2-D1. BRD4 D1-IN-3 reduces the expression of pro-inflammatory chemokines CXCL1 and CCL2 in an LPS (HY-D1056)-mediated cellular model of liver inflammation. BRD4 D1-IN-3 can be used for liver inflammation research.
    BRD4 D1-IN-3
  • HY-152471
    Eleven-Nineteen-Leukemia Protein IN-3
    		Inhibitor
    Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro.
    Eleven-Nineteen-Leukemia Protein IN-3
  • HY-142772
    Y08284
    		Inhibitor
    Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity.
    Y08284
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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