A cell-permeable azobenzene compound that reversibly targets CREB-binding protein bromodomain (CBP-BRD) acetyl-lysine binding pocket (=19uM) with moderate selectivity over BAZ1B, PCAF, BRD4-1 and BAZ2B ( = 37, 41, 70 and >100uM, 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=5uM for p53-induced p21 activation in Luc-U2OS cells) and suppress cardiac myocyte apoptosis during ischemia conditions.
Formula:C15H17N3SO4
Molecular Weight:335.4
Solubility:DMSO (50mg/ml, orange solution)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
