BI-9B12 White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A benzodioxane containing 2,4-disubstituted thiazolo compound that acts as a selective, reversible and competitive inhibitor of caspases (Ki = 4.3 µM, 6.2 µM and 2.7 µM for caspase-3, -7 and -8, respectively). The benzodioxane moiety is shown to fit in the 'aspartate hole' of the caspases and possibly disrupt caspase-8 assisted cleavage of BID, a proapoptotic protein. Weakly affects the activity of anthrax lethal factor, a metalloprotease, at ~20 µM. Purity: ≥97% by HPLC. Bl-9B12 Ref.: Fattorusso, R., et al. 2005. J. Med. Chem. 48, 1649. |
