A cell-permeable azobenzene compound that reversibly targets CBP-BRD acetyl-lysine binding pocket with moderate selectivity over BAZ1B, PCAF, BRD4-1 and BAZ2B.
别名:
Ischemin, (E)-5-(2-Amino-4-hydroxy-5-methyl-phenylazo)-2,4-dimethyl-benzenesulfonic acid, MS120, BRD4 Inhibitor II
A cell-permeable azobenzene compound that reversibly targets CREB-binding protein bromodomain (CBP-BRD) acetyl-lysine binding pocket (Kd = 19 µM) with moderate selectivity over BAZ1B, PCAF, BRD4-1 and BAZ2B (Kd = 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.
包装
Packaged under inert gas
警告
Toxicity: Regulatory Review (Z)
其他说明
Borah, J.C., et al. 2011, Chem. Biol.18, 531.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany