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.

Epigenetic Reader Domain Isoform Specific Products:

Epigenetic Reader Domain Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • 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-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-180152
    BRD4 ligand 14
    		Inhibitor
    BRD4 ligand 14 (Compound Y47) is a BRD4 inhibitor. BRD4 ligand 14 exhibits mild anticancer properties against acute myeloid leukemia by inhibiting BRD4. BRD4 ligand 14 can also be used as a ligand for target protein for PROTAC in the development and design of PROTAC BRD4 degraders, such as PROTAC BRD4 Degrader-42 (HY-180150).
    BRD4 ligand 14
  • 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-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-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-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-183248
    BRDT-IN-2
    		Inhibitor
    BRDT-IN-2 is a BRDT-BD1-preferring inhibitor (Ki=10 μM) with higher affinity for BRDT-BD1 than BRD4-BD1. BRDT-IN-2 preferentially binds BRDT-BD1 without direct interaction with BRDT-BD1’s Arg54 residue. BRDT-IN-2 binds BRD4-BD1 with lower affinity via structured water molecule displacement in its binding pocket. BRDT-IN-2 can be used for the research of multiple myeloma.
    BRDT-IN-2
  • 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
  • HY-143317
    XY153
    		Inhibitor
    XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer.
    XY153
  • HY-170686
    BRD4 Inhibitor-38
    		Inhibitor
    BRD4 Inhibitor-38 (Compound 25) is an orally active inhibitor of BRD4 with IC50 values of 3.64 μM and 0.12 μM against BRD4 BD1 and BRD4 BD2, respectively. BRD4 Inhibitor-38 also exhibits anti-inflammatory activity, with an IC50 value of 1.98 μM for inhibiting nitric oxide (NO) production.
    BRD4 Inhibitor-38
  • HY-163413
    BRD4-BD1-IN-3
    		Inhibitor
    BRD4-BD1-IN-3 (Compound 4g) is a BRD4-BD1 inhibitor. BRD4-BD1-IN-3 can be used for research of inflammatory disease.
    BRD4-BD1-IN-3
  • HY-168255
    PROTAC BRM/BRG1 degrader-4
    		Inhibitor
    PROTAC BRM/BRG1 degrader-4 (example 047) is a potent BRM and BRG1 PROTAC degrader, with DC50 values of 0.21 nM and 3.4 nM in SW1573 cells, respectively (Pink: ligand for target protein (HY-168252); Black: linker (HY-28911); Blue: E3 ligase ligand (HY-168253)).
    PROTAC BRM/BRG1 degrader-4
  • HY-174812
    BRD4 ligand 8
    		Inhibitor
    BRD4 ligand 8 (Compound J558) is a BRD4 inhibitor. BRD4 ligand 8 can be used for synthesis of PROTAC BRD4 Degrader-33 (HY-174811).
    BRD4 ligand 8
  • HY-N10802
    6-O-Isobutyrylbritannilactone
    		Inhibitor 98.34%
    6-O-Isobutyrylbritannilactone is a natural melanogenesis inhibitor. 6-O-Isobutyrylbritannilactone, a sesquiterpene, can be isolated from the flowers of Inula britannica. 6-O-Isobutyrylbritannilactone inhibits IBMX (HY-12318)-induced melanin production in B16F10 cells. 6-O-Isobutyrylbritannilactone also regulates ERK, PI3K/AKT, and CREB, shows antimelanogenic activity in zebrafish embryos models.
    6-O-Isobutyrylbritannilactone
  • HY-161498
    XYD198
    		Inhibitor
    XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161499))
    XYD198
  • HY-163543
    Progranulin modulator-2
    		Inhibitor
    Progranulin modulator-2 (compound 18A) is a bromodomain and extra-terminal domain (BET) inhibitor. Progranulin modulator-2 enhances PGRN expression by targeting members of the BET protein family. Progranulin modulator-2 can be used to study the role of BET protein in neurodevelopment, neuroplasticity and neurodegeneration.
    Progranulin modulator-2
Cat. No. Product Name / Synonyms Application Reactivity
Epigenetic Reader Domain Isoform Comparison

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