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Description

A cell-permeable azobenzene compound that reversibly targets CREB-binding protein bromodomain (CBP-BRD) acetyl-lysine binding pocket (Kd = 19 µ,M) with moderate selectivity over BAZ1B, PCAF, BRD4-1 and BAZ2B (Kd = 37, 41, 70 and >100 µ,M, respectively) and disrupts CBP interaction with the binding partners. Blocks CBP-p53 interaction and alters the post-translational modification states on p53 and histones. Shown to inhibit the transcription functions of p53 on DNA damage (IC50 = 5 µ,M for p53-induced p21 activation in Luc-U2OS cells) and suppress cardiac myocyte apoptosis during ischemia conditions.