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-P10894
    mUNO
    mUNO is a tumor-homing peptide (mUNO, sequence: "CSPGAK") that specifically binds to mouse CD206, targeting tumor-associated macrophages that express CD206/MRC1. mUNO can interact with human recombinant CD206.
    mUNO
  • 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-176056
    Hedgehog IN-9
    		Agonist
    Hedgehog IN-9 (Compound 1) is a Hedgehog inhibitor. Hedgehog IN-9 prevents GLI1 expression and enhances cellular BRD2 protein levels. Hedgehog IN-9 inhibits growth of medulloblastoma spheroid cells and can be used for synthesis of photoaffinity labeling probe.
    Hedgehog IN-9
  • 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 (compound 15) is a potent PBRM1 Bromodomain inhibitor with Kd values of 5.5 μM and 11.1 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.2 μM for PBRM1-BD2. PBRM1-BD2-IN-4 can be used to research anticancer.
    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-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-155393
    PROTAC BRD4 Degrader-22
    		Inhibitor
    PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based BRD4 degrader, with a pDC50 (MOLT4, 24 h) of 9.2.
    PROTAC BRD4 Degrader-22
  • 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-173256
    Hyp-dBET1
    		Degrader
    Hyp-dBET1 is a PROTAC degrader targeting BRD4. Hyp-dBET1 has an IC50 value of 3.4 μM in MDA-MB-231 cells. Hyp-dBET1 can be activated by hypoxia and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study.
    Hyp-dBET1
  • HY-177729
    PROTAC BRD9 Degrader-9
    		Degrader
    PROTAC BRD9 Degrader-9 is an efficient and selective targeting BRD9 PROTAC degrader. PROTAC BRD9 Degrader-9 does not cause significant cytotoxicity. PROTAC BRD9 Degrader-9 can be used for cancer research. (Pink: BRD9 Ligand (HY-107446); Blue: CRBN Ligand (HY-W877239))
    PROTAC BRD9 Degrader-9
  • HY-124859
    CeMMEC2
    CeMMEC2 is a direct BRD4 inhibitor with an IC50 of 0.9 μM.
    CeMMEC2
  • HY-160670
    BRD4-IN-6
    		Inhibitor
    BRD4-IN-6 (compound 116) is a BRD4 inhibitor (extracted from patent CN107721975A).
    BRD4-IN-6
  • HY-162748
    PROTAC SMARCA2/4-degrader-30
    		Degrader
    PROTAC SMARCA2/4-degrader-30 (Compound I-291) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-30 degrades SMARCA2 in A549 and in MV411 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: ligand for target protein (HY-163926); Black: linker (HY-159684); Blue: ligand for E3 ligase (HY-W382038)).
    PROTAC SMARCA2/4-degrader-30
  • HY-177730
    PROTAC BRD4 Degrader-40
    		Degrader
    PROTAC BRD4 Degrader-40 is a Bromodomain protein 4 (BRD4) PROTAC degrader. PROTAC BRD4 Degrader-40 can induce BRD4 degradation in cancer cells. PROTAC BRD4 Degrader-40 can be used for the research of cancer, such as leukemia. (Structure Note: Pink: BRD4 ligand (HY-78695); Blue: CRBN ligand (HY-163927))
    PROTAC BRD4 Degrader-40
  • HY-111978
    ZEN-3862
    		Inhibitor 98.86%
    ZEN-3862 is a BET inhibitor with IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively. ZEN-3862 can be used to form PROTACs to induce degradation of BRD4.
    ZEN-3862
Cat. No. Product Name / Synonyms Application Reactivity