A p300 and CBP inhibitor
cAMP-responsive element-binding protein binding protein (CREBBP) and E1A-associated protein p300 (EP300) are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development. Both CBP and EP300 contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins. I-CBP112 is a selective inhibitor of CBP and EP300 that directly binds their bromodomains (Kds = 0.142 and 0.625 μM, respectively). Developed by the Structural Genomics Consortium (SGC), this compound shows only weak cross-reactivity with the bromodomains of bromodomain and extra-terminal proteins and shows no interaction with other bromodomains.
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