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-164005
    CBP/EP300 bromodomain receptor-IN-1
    		Inhibitor
    CBP/EP300 bromodomain receptor-IN-1 (Compound 10) is an inhibitor for CBP/EP300 bromodomain receptor, which binds to proteins having a bromodomain in nanomolar level.
    CBP/EP300 bromodomain receptor-IN-1
  • HY-162622
    BET-IN-26
    		Inhibitor
    BET-IN-26 (compound 13a) is a potent, selective and orally active BD1 inhibitor with IC50 values of 0.0055, 9.0 µM for BD1, BD2, respectively. BET-IN-26 decreases LPS (HY-D1056) induced serum levels of IL-6 and MCP-1.
    BET-IN-26
  • HY-173255
    DAO-dBET1
    		Degrader
    DAO-dBET1 is a Dual-Action-Only PROTAC containing a PROTAC degrader, dBET1 (HY-101838). DAO-dBET1 is a potent BRD4 degrader with a DC50 value of 277 nM in the presence of CoCl2. DAO-dBET1 inhibits hypoxia and Cath-L trigger with an IC50 value of 281 nM.
    DAO-dBET1
  • HY-174450
    KMT9-IN-1
    		Inhibitor
    KMT9-IN-1 (Compound 8) is a KMT9 inhibitor and the ethyl ester prodrug of compound 7b. KMT9-IN-1 releases the active form 7b via esterases in cells. KMT9-IN-1 targets KMT9 in cells and reduces H4K12me1 levels. KMT9-IN-1 has antitumor activity against colon cancer. KMT9-IN-1 can be used in the research of prostate cancer and hepatocellular carcinoma.
    KMT9-IN-1
  • HY-152213
    BET-IN-13
    		Inhibitor
    BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury.
    BET-IN-13
  • HY-170900
    SJ44236
    		Degrader
    SJ44236 is the PROTAC degrader for BET that degrades BRD2 (DC50 = 0.127 nM), BRD3 and BRD4. SJ44236 exhibits cytotoxicity in cell MV4-11 and HD-MB03 with IC50s of 0.12 nM and 0.92 nM. SJ44236 downregulates the expression of c-Myc, upregulates the expression of p53. SJ44236 exhibits a good orally bioavailability of 45% in mice. (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W012935); Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 54 (HY-W890189))
    SJ44236
  • HY-120196
    CPI703
    		Inhibitor
    CPI703, a BRD inhibitor, binds with residues in domain1 of 5DBM complex.
    CPI703
  • HY-W010649R
    Isoxazole (Standard)
    		Inhibitor
    Amfenac (Sodium Hydrate) (Standard) is the analytical standard of Amfenac (Sodium Hydrate). This product is intended for research and analytical applications. Amfenac Sodium Hydrate is a COX-2 inhibitor.
    Isoxazole (Standard)
  • HY-163877
    PROTAC SMARCA2/4-degrader-19
    		Degrader
    PROTAC SMARCA2/4-degrader-19 (Compound I-412) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-19 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-163949); Black: Linker (HY-W006635); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-19
  • HY-117598
    OXFBD03
    OXFBD03 serves as an inhibitor of the BRD4(1) protein, which belongs to the bromodomain and extra terminal domain bromodomain family.
    OXFBD03
  • HY-163639
    BRD4 degrader-2
    		Inhibitor
    BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells.
    BRD4 degrader-2
  • HY-19549
    RX-37
    		Inhibitor
    RX-37 is a selective BET inhibitor. RX-37 binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with Ki values of 3.2-24.7 nM. RX-37 can be used for research of cancers.
    RX-37
  • HY-168448
    dBAZ2
    		Degrader
    dBAZ2 is a first-in-class BAZ2A and BAZ2B PROTAC degrader with DC50 values of 180 nM and 250 nM for BAZ2A and BAZ2B, respectively. (Blue: E3 ligase ligand (VH 101, thiol (HY-47851); Black: linker (HY-168450); pink: target protein ligand (HY-168449)).
    dBAZ2
  • HY-149735
    BET-IN-20
    		Inhibitor
    BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage.
    BET-IN-20
  • HY-175240
    PROTAC BRD4 Degrader-38
    		Degrader
    PROTAC BRD4 Degrader-38 is a BRD4 PROTAC degrader with DC50s of 86 and 106 nM for the short and long isoforms of BRD4, respectively. PROTAC BRD4 Degrader-38 significantly induces the degradation of BRD4 by covalently engaging C232 of E3 ligase TRIM28.Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-203082); Black: linker (HY-40172)
    PROTAC BRD4 Degrader-38
  • HY-173062
    BRD4 Inhibitor-40
    		Inhibitor
    BRD4 Inhibitor-40 (Compound 23) is the inhibitor for BRD that inhibits BRD4-BD1, BRD4-BD2, BRD2-BD1 and BRD2-BD2 with IC50s of 16.1, 142.18, 29.35 and 302.35 nM, respectively. BRD4 Inhibitor-40 modulates the expression of c-Myc and p21, arrests cell cycle at G1 phase, inhibits Pkd1-null (PN) renal cystic epithelial cells, and blocks the renal cysts formation in Madin-Darby canine kidney and embryonic kidney vesicle models. BRD4 Inhibitor-40 exhibits renal cysts inhibitory activity in mouse models.
    BRD4 Inhibitor-40
  • HY-N16129
    Diplacone
    		Inducer
    Diplacone (DP) is a geranylated flavanone. Diplacone can be isolated from the unripe fruits of Paulownia tomentosa. Diplacone has anti-inflammatory, antiradical, cytoprotective, antibacterial and anticancer activities. Diplacone induces ferroptosis-mediated cell death by increasing mitochondrial Ca2+ Influx, ROS production and mitochondrial permeability transition. Diplacone significantly inhibits AChE and BChE activity with IC50s of 7.2  μM and 1.4 μM for hAChE and BChE, respectively. Diplacone can be used for chronic inflammatory diseases like inflammatory bowel diseases (IBD), cancers like lung cancer and Alzheimer’s disease research.
    Diplacone
  • HY-160262
    AR/BET protein degrader-1
    		Degrader
    AR/BET protein degrader-1 (Compound 149) is an Androgen Receptor and BET (bromodomain and extra-terminal domain) protein degrader that can be used in cancer research.
    AR/BET protein degrader-1
  • HY-174996
    NEP162
    		Degrader
    NEP162 is a BRD4 PROTAC degrader with DC50s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc. (Pink: BRD4 ligand : (HY-78695), Blue: E3 ligase Ligand (HY-D2259), BLACK: Linker, E3 ligase ligand-linker conjugate (HY-174997)).
    NEP162
  • HY-177143
    CDD-1498
    		Inhibitor
    CDD-1498 (Compound 12) is a potent inhibitor of BRDT-BD2. CDD-1498 has an IC50 of 978 nM against BRDT-BD2. CDD-1498 can be studied in research on nonhormonal contraceptive agent.
    CDD-1498
Cat. No. Product Name / Synonyms Application Reactivity