Ischemin, CBP Bromodomain Inhibitor


Catalog No. size PriceQuantity
M60229-2S 2 mg solid $79
M60229-10S 10 mg solid $312

Description

Product Information
Molecular Weight: 357.36
Formula: C15H16N3O4SNa
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 100 mM
Chemical Name: sodium (E)-5-((2-amino-4-hydroxy-5-methylphenyl)diazenyl)-2,4-dimethylbenzenesulfonate
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

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. 



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