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-142952
    UNC6864 (Kei)
    		Inhibitor
    UNC6864 (Kei), an ethylisopropyllysine (Kei)-containing ligand, binds to wild-type CBX5, with a KD of 3.3 μM.
    UNC6864 (Kei)
  • HY-163868
    PROTAC SMARCA2/4-degrader-15
    		Degrader
    PROTAC SMARCA2/4-degrader-15 (Compound I-335) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-15 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-N3024); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-15
  • HY-159461
    PROTAC SMARCA2/4-degrader-9
    		Degrader
    PROTAC SMARCA2/4-degrader-9 (Compound I-503) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2 degrader-9 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W006635); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-9
  • HY-178490
    BRM/BRG1 ATP-IN-8
    		Inhibitor
    BRM/BRG1 ATP-IN-8 (Compound Cpd14) is an orally active BRG1/BRM ATPase domain inhibitor. BRM/BRG1 ATP-IN-8 exerts antitumor effects by disrupting aberrant chromatin remodeling in cancer cells, inducing apoptosis and growth arrest. BRM/BRG1 ATP-IN-8 is promising for research of BRG1/BRM-dependent malignancies, including hematological cancers, prostate cancer, breast cancer, and Ewing's sarcoma.
    BRM/BRG1 ATP-IN-8
  • HY-170989
    BRD4 degrader-5
    		Degrader
    BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC50 = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC50 of 20.6 μM.
    BRD4 degrader-5
  • HY-146292
    BET-IN-8
    		Inhibitor
    BET-IN-8 (Compound 27) is a potent inhibitor of BET with a Ki and Kd of 0.83 and 0.571 μM, respectively. BET-IN-8 ameliorates LPS-induced sepsis in vivo. BET-IN-8 has the potential for the research of sepsis.
    BET-IN-8
  • HY-174210
    PROTAC BRD4 Degrader-31
    		Degrader
    PROTAC BRD4 Degrader-31 is a BRD4 PROTAC degrader with DC50 s of 164 and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-31 potently degrades BRD4 in cells with long acting degradation kinetics. Pink: BRD4 ligand (HY-78695); Blue: KLHDC2 ligand (HY-174218)
    PROTAC BRD4 Degrader-31
  • HY-169274
    PROTAC SMARCA2 degrader-23
    		Degrader
    PROTAC SMARCA2 degrader-23 (Example 1) is a potent and selective PROTAC SMARCA2 degrader，with a DC50 of <100 nM. PROTAC SMARCA2 degrader-23 has the potential for the research of cancer.
    PROTAC SMARCA2 degrader-23
  • HY-138637
    PROTAC BRD4 Degrader-14
    		Inhibitor
    PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
    PROTAC BRD4 Degrader-14
  • HY-151894
    I-BET432
    		Inhibitor
    I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases.
    I-BET432
  • HY-P5763A
    Phoenixin-20 TFA
    Phoenixin-20 (TFA) (PNX-20 (TFA)) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. Phoenixin-20 (TFA) promotes neuronal mitochondrial biogenesis via CREB-PGC-1α pathway. Phoenixin-20 (TFA) has anxiolytic effect.
    Phoenixin-20 TFA
  • HY-12421B
    BET-BAY 002 (S enantiomer)
    BET-BAY 002 S enantiomer is the S-enantiomer of BET-BAY 002. BET-BAY 002 is a BET inhibitor.
    BET-BAY 002 (S enantiomer)
  • HY-153414
    GXF-111
    		Degrader
    GXF-111, a PROTAC molecule, can promote selective degradation of cellular BRD3 and BRD4-L. GXF-111 has binding affinities for BRD3 BD1 and BRD3 BD2 with Ki values of 11.97 nM and 2.35 nM, respectively. GXF-111 can be used for the research of cancer.
    GXF-111
  • HY-162739
    SMARCA2-IN-1
    		Inhibitor
    SMARCA2-IN-1 (Compound I-19) is an inhibitor for SWI/SNF chromatin remodeling complexe SMARCA2 with IC50 >1000 nM in H1299.
    SMARCA2-IN-1
  • HY-P11217
    MACTIDE
    MACTIDE is a CD206 targeting peptide with high affinity and stability. MACTIDE is commonly used to enhance the targeting of drugs. MACTIDE can be used in the research of cancer such as breast cancer.
    MACTIDE
  • HY-160672
    BRD4-IN-8
    		Inhibitor
    BRD4-IN-8 (Example 13b) is a BRD4 inhibitor.
    BRD4-IN-8
  • HY-177124
    Repibresib
    		Inhibitor
    Repibresib (VYN201) is a bromodomain and extra-terminal motif (BET) inhibitor. Repibresib shows antineoplastic activity.
    Repibresib
  • HY-153751
    BRD4-IN-4
    BRD4-IN-4 (Compound 1) is a BRD4 inhibitor (IC50=6.83 μM). BRD4-IN-4 selectively inhibits MV4-11 cell line proliferation and arrests cell at G1 phase. BRD4-IN-4 can be used for research of MLL leukemia.
    BRD4-IN-4
  • HY-120245
    GSK-340
    GSK-340 is a BET inhibitor with high affinity and significant selectivity for BD2 from BRD4 with a pIC50 of 7.2. GSK-340 inhibits MCP-1 release in Lipopolysaccharide (HY-D1056) treated PBMCs and whole blood with the pIC50 of 7.4 and 6.0, respectively. GSK-340 has immunomodulatory activity.
    GSK-340
  • HY-170453
    iHAC
    		Degrader
    iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models.
    iHAC
Cat. No. Product Name / Synonyms Application Reactivity