Ischemin is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin inhibits p53 -induced p21 activation with an IC50 value of 5 µM. Ischemin also prevents apoptosis in ischemic cardiomyocytes. Ischemin can be used in the study of cardiovascular diseases (such as myocardial ischemia) [1].
In Vitro, Ischemin (50, 100 µM; 24 h) inhibits p53 activation on DNA damaging stress in U2OS cells[1]. Ischemin (10 μM; 3 days) blocks apoptosis in cardiomyocytes by inhibiting caspase 3/7 activity[1]. Ischemin inhibits p53 cellular signaling pathways in U2OS cells[1].
References:
[1]. Borah JC, et al. A small molecule binding to the coactivator CREB-binding protein blocks apoptosis in cardiomyocytes. Chem Biol. 2011 Apr 22;18(4):531-41.
In Vitro, Ischemin (50, 100 µM; 24 h) inhibits p53 activation on DNA damaging stress in U2OS cells[1]. Ischemin (10 μM; 3 days) blocks apoptosis in cardiomyocytes by inhibiting caspase 3/7 activity[1]. Ischemin inhibits p53 cellular signaling pathways in U2OS cells[1].
References:
[1]. Borah JC, et al. A small molecule binding to the coactivator CREB-binding protein blocks apoptosis in cardiomyocytes. Chem Biol. 2011 Apr 22;18(4):531-41.