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Epigenetic Reader Domain

Epigenetic reader domain inhibitors, mostly bromodomain inhibitors, block recognition of acetylated histone lysines. Structural work on a histone acetyltransferase bromodomain first showed that this module binds acetylated lysine. Proteins of the bromodomain and extra-terminal (BET) family, such as bromodomain-containing protein 4 (BRD4), link histone acetylation to gene transcription. The thienodiazepine (+)-JQ1 was described in 2010 as a selective BET inhibitor that displaces BRD4 from chromatin. PFI-1, GSK1324726A and CPI-203 provide further BET inhibitor chemotypes for comparative studies. Other entries reach beyond BET binding, such as SGC-CBP30 for a non-BET bromodomain and the BRD4-degrading compound ARV-825.

3 Items

  • 653-47 hydrochloride
    Cat. No.
    A24421
    CAS No.
    1224567-46-7

    653-47 hydrochloride

    653-47 hydrochloride is a potentiator that significantly enhances the CREB (cAMP-response element-binding protein) inhibitory activity of 666-15. It also functions as a very weak CREB inhibitor on its own, with an IC₅₀ of 26.3 μM.

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    5 mg
    $198.00
    10 mg
    $341.00
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  • UNC4976
    Cat. No.
    A26805
    CAS No.
    2920299-34-7

    UNC4976

    UNC4976 is a positive allosteric modulator of the CBX7 chromodomain, targeting nucleic acid binding. It functions by antagonizing the H3K27me3-specific recruitment of CBX7 to target genes while enhancing non-specific binding to DNA and RNA. This compound is valuable for research focused on chromatin regulation and the epigenetic mechanisms involved in gene expression.

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