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Bromodomain(BRD)


A bromodomain is an approximately 110 amino acid protein domain that recognizes acetylated lysine residues, such as those on the N-terminal tails of histones. Bromodomains are responsible in transducing the signal carried by acetylated lysine residues and translating it into various normal or abnormal phenotypes. Bromodomain-containing proteins can have a wide variety of functions, ranging from histone acetyltransferase activity and chromatin remodeling to transcriptional mediation and co-activation.
  • I-BET-762 EY1664

    I-BET-762是一种BET (bromodomain and extra terminal domain)蛋白抑制剂, IC50约为35 nM,抑制巨噬细胞产生促炎蛋白,抑制急性炎症,对其他溴区结合域包含的蛋白具有高度的选择性。

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  • PFI-1 EY1601

    PFI-1 (PF-6405761)是一种选择性的BET(溴区包含蛋白)抑制剂,抑制BRD4时IC50为0.22 μM。

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  • RVX-208 EY1175

    RVX-208是一种有效的BET bromodomain抑制剂,作用于BD2, IC50为0.510 μM,比作用于BD1选择性高170倍。

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  • SGC-CBP30 EY0815

    SGC-CBP30是CREBBP和EP300的布罗莫结构域抑制剂,IC50分别为21-69nM和38 nM。

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  • I-BET151 EY0823

    I-BET151(GSK1210151A)是BET布罗莫结构域抑制剂,对BRD4的pIC50为6.1。

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