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Biological Activity:

Ischemin is a potent, selective and cell permeable CBP bromodomain inhibitor. It inhibits the acetyl-lysine binding activity of the bromodomain of CBP. It alters post-translational modifications on p53 and histones, inhibits p53 interaction with CBP and transcriptional activity in cells, and prevents Doxorubicin-induced apoptosis in ischemic cardiomyocytes. Ischemin is a good chemical probe to modulate acetylation-mediated interactions in gene transcription and a new approach to therapeutic interventions of human disorders such as myocardial ischemia


How to Use:

In vitro: Ischemin was used at 10-50 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Borah JC, et al. A small molecule binding to the coactivator CREB-binding protein blocks apoptosis in cardiomyocytes. (2011) Chem Biol. 18(4):531-41.