General description

A cell-permeable azobenzene compound that reversibly targets CREB-binding protein bromodomain (CBP-BRD) acetyl-lysine binding pocket (K_d = 19 µM) with moderate selectivity over BAZ1B, PCAF, BRD4-1 and BAZ2B (K_d = 37, 41, 70 and >100 µM, 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 µM for p53-induced p21 activation in Luc-U2OS cells) and suppress cardiac myocyte apoptosis during ischemia conditions.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Borah, J.C., et al. 2011, Chem. Biol.18, 531.

Packaging

25 mg in Glass bottle

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)