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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.

Products Related to Epigenetic Reader Domain(298)

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    dBRD9 is a BRD9 PROTAC degrader.

  • GC84862 structure
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    Curcumin -d 6 (Diferuloylmethane-d 6 ) is deuterium labeled Curcumin.

  • GC84901 structure
    GC84901BET bromodomain-IN-5
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    BET bromodomain-IN-5 is an orally active BET inhibitor with an IC 50 of 14 nM against BRD4 (1).

  • GC84974 structure
    GC84974TEC 4
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    TEC 4 is a ByeTAC (Bypassing E-Ligase-Targeting Chimera) BRD4 degrader, with 33% BRD4 remaining at 500 nM in Ramos B-cells.

  • GC84984 structure
    GC84984YTH-IN-1
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    YTH-IN-1 (compound N-7) is a pan- YTH domain inhibitor with the IC 50 values of 39 μM, 34 μM, 35 μM, 48 μM and 30 μM for human YTH YTHDF1, YTH YTHDF2, YTH YTHDF3, YTH YTHDC1, and YTH YTHDC2, respectively [1] .

  • GC10174 structure
    GC10174SGC-CBP30
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    Purity: >99.50%

    SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain inhibitor, with K d values of 21nM and 32nM for CBP and p300, respectively.

  • GC10382 structure
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    CBP/EP300 bromodomain inhibitor

  • GC10402 structure
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    A non-specific bromodomain inhibitor

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    An inhibitor of menin-MLL fusion protein interactions

  • GC11439 structure
    GC11439MG 149
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    Purity: >98.00%

    MG 149 is an inhibitor of histone acetyltransferases (HAT) with IC 50 values of 74μM and 47μM for Tip60 and MOF, respectively.

  • GC12199 structure
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    An inhibitor of menin-MLL fusion protein interactions

  • GC12419 structure
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  • GC12440 structure
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  • GC12450 structure
    GC12450BI 2536
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    Purity: >98.00%

    BI 2536, dual Polo-like kinase (PLK)/bromodomain inhibitors, effectively reactivate latent HIV-1. Half maximal inhibitory concentration (IC 50 ) values of BI 2536 against PLK1, PLK2, and PLK3 in cell-free kinase assays are 0.83nM, 3.5nM and 9.0nM, respectively.

  • GC12588 structure
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    BRD9 inhibitor

  • GC12733 structure
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    Purity: >98.00%

    C646, a potent and selective p300/CBP histone acetyltransferase inhibitor (Ki 400 nM), has been shown to have pleiotropic activity, including neuroprotective, anti-cancer and anti-epithelial-mesenchymal transition (anti-EMT) effects.

  • GC13025 structure
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    Purity: >99.00%

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  • GC13822 structure
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    A selective inhibitor of BET bromodomains

  • GC14063 structure
    GC14063GSK1324726A
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    Purity: >98.00%

    BET proteins inhibitor

  • GC14103 structure
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    Purity: >98.00%

    EGFR activator

  • GC14199 structure
    GC14199RVX-208
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    Purity: >99.00%

    RVX-208 (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87 μM and 0.51 μM for BD1 and BD2, respectively.

  • GC14361 structure
    GC14361PFI 3
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    Purity: >98.00%

    inhibitor of polybromo 1 and SMARCA4