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.

1 Item

  • MZ1
    Cat. No.
    A17014

    MZ1

    MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3.

    1 mg
    $40.00
    2 mg
    $75.00
    All 7 sizes

1 Item

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