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-143270
    PROTAC BRD9-binding moiety 5
    PROTAC BRD9-binding moiety 5 is a selective BRD9 binder with an IC50 value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells.
    PROTAC BRD9-binding moiety 5
  • HY-147869
    DC-CPin7
    		Inhibitor
    DC-CPin7 is a potent inhibitor of CREB-binding protein (CBP) bromodomain with an IC50 of 2.5 μM.
    DC-CPin7
  • HY-159455
    PROTAC SMARCA2/4-degrader-4
    		Degrader
    PROTAC SMARCA2/4-degrader-4 (Compound I-434) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-4 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-159472); Black: Linker (HY-159478); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-4
  • HY-176477
    BRD4/FKBP12 degrader-2
    		Degrader
    BRD4/FKBP12 degrader-2 (a1dj) is a BRD4/FKBP12 degrader and shows anticancer activity (BRD4 ligand: HY-78695, FKBP12 ligand: HY-176502, linker: HY-140212).
    BRD4/FKBP12 degrader-2
  • HY-175179
    LO-3-61
    		Degrader
    LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells.
    LO-3-61
  • HY-159602
    BET BD2-IN-3
    		Inhibitor
    BET BD2-IN-3 (compound I-58) is an inhibitor of BET, targeting the BD2 domain of BET. BET BD2-IN-3 can be radiolabeled with [11C] for positron emission tomography (PET) imaging. BET [11C]BD2-IN-3 showed suitable biodistribution in peripheral organs and tissues in PET applications in mice.
    BET BD2-IN-3
  • HY-163271
    XL-126
    		Inhibitor
    XL-126 (Compound 33) is a potent BD1-selective BET inhibitor, with a Kd of 8.9 nM. XL-126 leads to both the preservation of platelets and potent anti-inflammatory efficacy by BD1 selectivity.
    XL-126
  • HY-117690A
    dBRD9 dihydrochloride
    		Degrader
    dBRD9 dihydrochloride is a selective BRD9 PROTAC degrader. dBRD9 dihydrochloride inhibits proliferation of AML cell lines.
    dBRD9 dihydrochloride
  • HY-168464
    Y16526
    		Inhibitor
    Y16526 is a potent inhibitor of CBP/p300 bromodomain , with the IC50 of 0.03 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).
    Y16526
  • HY-169488
    SMARCA2 ligand-12-3-methylazetidine
    		Inhibitor
    SMARCA2 ligand-12-3-methylazetidin is a target protein ligand-linker conjugate that incorporates a ligand for SMARCA2 (HY-169487), and a PROTAC linker (HY-W052601), which recruit E3 ligases. SMARCA2 ligand-12-3-methylazetidin can be used to synthesize PROTAC SMARCA2 degrader-25 (HY-169276).
    SMARCA2 ligand-12-3-methylazetidine
  • HY-171774
    PBRM1/SMARCA2,4-ligand-1
    PBRM1/SMARCA2,4-ligand-1 (Compound 4) is a Ligand for Target Protein for PROTAC that binds to PBRM1, SMARCA2, and SMARCA4. PBRM1/SMARCA2,4-ligand-1 is a potent SMARCA4 bromodomain inhibitor. PBRM1/SMARCA2,4-ligand-1 can be used to synthesize PROTAC AU-24118 (HY-163410).
    PBRM1/SMARCA2,4-ligand-1
  • HY-N16067
    Penipanoid C
    		Inhibitor
    Penipanoid C (Compound 9) is a BRD4 inhibitor. Penipanoid C can be isolated from marine sediment-derived fungus Penicillium paneum SD-44. Penipanoid C has anti-inflammatory activity and cytotoxic activity against the SMMC-7721 cells. Penipanoid C can be used for inflammatory diseases research.
    Penipanoid C
  • HY-117948
    ML399
    		Inhibitor
    ML399 is a Menin-Mixed Lineage Leukemia (MLL) protein-protein interaction inhibitor.
    ML399
  • HY-162834
    PROTAC SMARCA2/4-degrader-27
    		Degrader
    PROTAC SMARCA2/4-degrader-27 (PROTAC 2) is a PROTAC-based degrader of SMARCA2 and SMARCA4. (Blue: CRL2VHL ligand VH032-cyclopropane-F (HY-125905); Black: linker (HY-159678);Pink: a SMARCA-BD ligand 1 for PROTAC (HY-44012)).
    PROTAC SMARCA2/4-degrader-27
  • HY-162621
    BET-IN-25
    		Inhibitor
    BET-IN-25 (compound 7) is an oral bioactive inhibitor of bromodomain (BD1) and BD2, with the IC50s of 0.18 μM and 9.2 μM, respectively.
    BET-IN-25
  • HY-175679
    BRD2 BD1 ligand-1
    		Ligand
    BRD2 BD1 ligand-1 is a potent BRD2 BD1 ligand (Ligands for Target Protein for PROTACs) can be used in the synthesis of PROTAC BRD2 BD1 Degrader-1 (HY-175678).
    BRD2 BD1 ligand-1
  • HY-P10947
    MACTIDE-V
    		Inhibitor
    MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206+ tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models.
    MACTIDE-V
  • HY-143300
    BRD4-BD1-IN-2
    		Inhibitor
    BRD4-BD1-IN-2 is a selective BRD4-BD1 inhibitor, with an IC50 of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases.
    BRD4-BD1-IN-2
  • HY-175611
    FLT3/JAK2/BRD4 ligand-1
    		Ligand
    FLT3/JAK2/BRD4 ligand-1 is a FLT3/JAK2/BRD4 ligand. FLT3/JAK2/BRD4 ligand-1 can be used for synthesis PROTAC FLT3/JAK2/BRD4 Degrader-1(HY-175610).
    FLT3/JAK2/BRD4 ligand-1
  • HY-168257
    PROTAC SMARCA2 degrader-30
    		Inhibitor
    PROTAC SMARCA2 degrader-30 (example 85) is a PROTAC SMARCA2 degrader with a DC50 less than 100 nM in H1299 cells.
    PROTAC SMARCA2 degrader-30
Cat. No. Product Name / Synonyms Application Reactivity