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-147571
    BET-IN-9
    		Inhibitor
    BET-IN-9 is a BET inhibitor extracted from patent WO2022012456A1, compound example 1.
    BET-IN-9
  • HY-143299
    BRD4-BD1-IN-1
    		Inhibitor
    BRD4-BD1-IN-1 (Compound 9a) is a BRD4-BD1 inhibitor with an IC50 of 38.20 μM.
    BRD4-BD1-IN-1
  • HY-138623
    GSK789
    		Inhibitor
    GSK789, a chemical probe, is an effective, cell-permeable, and highly selective inhibitor of the BET family first bromodomain (BD1), with antitumor and immunomodulatory effects
    GSK789
  • HY-163871
    PROTAC SMARCA2/4-degrader-18
    		Degrader
    PROTAC SMARCA2/4-degrader-18 (Compound I-348) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-18 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159531); Black: Linker (HY-76547); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-18
  • HY-161650
    PROTAC BRD4 Degrader-26
    		Degrader
    PROTAC BRD4 Degrader-26 (PROTAC-2) is a photo-regulated PROTAC, which degrades 80% BRD4 at 1 μM by using photocleavable linker. PROTAC BRD4 Degrader-26 will be deactivated by UV light. (Pink: ligand for target protein BRD4 ligand 6 (HY-161651); Black: linker (HY-161653); Blue: E3 ligase ligand Thalidomide 4-fluoride (HY-41547))
    PROTAC BRD4 Degrader-26
  • HY-163872
    PROTAC SMARCA2/4-degrader-10
    		Degrader
    PROTAC SMARCA2/4-degrader-10 (compound I-399) is a potent SMARCA2 degrader with an DC50 value of ＜100 nM. PROTAC SMARCA2/4-degrader-10 has the potential for the research of cancer (Blue:SMARCA2/4 ligand, (HY-159542); Black: linker (HY-W088435); Pink:VHL ligand (HY-125845)).
    PROTAC SMARCA2/4-degrader-10
  • HY-141438A
    cis-SIM1
    		Control
    cis-SIM1 is a negative control of SIM1.
    cis-SIM1
  • HY-160634
    BRD4 Inhibitor-31
    		Inhibitor
    BRD4 Inhibitor-31 (Example 136) is a BRD4 inhibitor (Kis: 0.234 μM and 0.295 μM for BRD4 BD1 and BRD4 BD2 respectively). BRD4 Inhibitor-31 can be used for research of inflammatory diseases, cancer, and AIDS.
    BRD4 Inhibitor-31
  • HY-155229
    CBP/p300-IN-21
    		Inhibitor
    CBP/p300-IN-21 (Compound 5d) is a selective CBP/p300 inhibitor (IC50: 0.07 and 1.755 μM for p300 and CBP). CBP/p300-IN-21 decreases H3K18Ac level. CBP/p300-IN-21 inhibits growth of 4T1 tumor growth in mice.
    CBP/p300-IN-21
  • HY-143328
    PROTAC BRD4 Degrader-17
    		Degrader
    PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells.
    PROTAC BRD4 Degrader-17
  • HY-141843
    BRD4-IN-2
    BRD4-IN-2 is a bromodomain BRD4 inhibitor with an IC50 value of 9.9 nM.
    BRD4-IN-2
  • HY-144236
    ZLD2218
    Considerable studies confirmed that BRD4 inhibition ameliorated kidney injury and fibrosis ，and ZLD2218 exhibited the most potent inhibitory activity against BRD4, with the IC50 value of 107 nM
    ZLD2218
  • HY-120772
    UNC-1679
    		Antagonist
    UNC-1679 is a L3MBTL3 antagonist (Kd: 0.47 μM for L3MBTL3, 68 μM for L3MBTL1).
    UNC-1679
  • HY-175756
    SMARCA2/4 degrader-1
    		Degrader
    SMARCA2/4 degrader-1 (Compound 1) is a SMARCA2/4 molecular glue degrader with a DC50 of 2.2  nM for SMARCA4. SMARCA2/4 degrader-1 covalently recruits both CUL4DCAF16 and CRL1FBXO22 to degrade SMARCA2/4.
    SMARCA2/4 degrader-1
  • HY-178345
    ZZ7-23-022
    		Degrader
    ZZ7-23-022 (ZZ7) is a selective BRD9 molecule glue degrader. ZZ7-23-022 effectively degrades BRD9 in synovial sarcoma cells, but does not affect cardiomyocytes. ZZ7-23-022 can be used for the research of cancer.
    ZZ7-23-022
  • HY-164098
    JWZ-7-7-Neg1
    		Inhibitor
    JWZ-7-7-Neg1 is a transcriptional chemical inducers of proximity (TCIP) with negative chemical control. JWZ-7-7-Neg1 reduces the ability to bind to BRD4 or BCL6, so it has less cytotoxicity to DLBCL cells, in compared with JWZ-7-7.
    JWZ-7-7-Neg1
  • HY-143339
    CBP/p300-IN-15
    		Inhibitor
    CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC50 values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC50 values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research.
    CBP/p300-IN-15
  • HY-153668A
    Bromodomain inhibitor-12 (edisylate)
    		Inhibitor
    Bromodomain inhibitor-12 edisylate (example 303) is a bromodomain inhibitor that can be used in the research of autoimmune and inflammatory diseases.
    Bromodomain inhibitor-12 (edisylate)
  • HY-176724
    ZnPc-O3-JQ1
    		Degrader
    ZnPc-O3-JQ1 is a light-triggered BRD4 degrader. Under illumination, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) that degrades BRD4. The degradation of BRD4 results in downregulation of HIF-1α, thereby counteracting the photodynamic therapy (PDT) resistance induced by tumor hypoxia. ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms. The structure of ZnPc-O3-JQ1 consists of three parts: BRD4 ligand (HY-78695); Linker (HY-W040165); Photosensitizer (HY-176725).
    ZnPc-O3-JQ1
  • HY-178043
    BTR2038
    		Degrader
    BTR2038 is a BRD9 degrader. BTR2038 induces targeted degradation of V5-tagged human BRD9. BTR2038 can be used for the study of biological processes and diseases associated with abnormal BRD9 protein function.
    BTR2038
Cat. No. Product Name / Synonyms Application Reactivity