Ivachtin is a potent inhibitor of caspase-3 with IC50 value of 23 nM .
Caspase-3 is a member of the cysteine-aspartic acid protease family and interacts with caspase-8 and caspase-9. Sequential activation of caspases plays an important role in cell apoptosis.
Ivachtin is a potent and reversible inhibitor of caspase-3 in a noncompetitive way. Ivachtin was the most potent inhibitor against caspase-3, but the selectivity versus the remaining caspases was modest. In human Jurkat T cells treated with 10 μM staurosporin, Ivachtin protected cells in a higher level, which suggested that Ivachtin had a good cell permeability and antiapoptotic activity .
. Kravchenko DV, Kuzovkova YA, Kysil VM, et al. Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors. J Med Chem, 2005, 48(11): 3680-3683.
|Physical Appearance||A crystalline solid|
|Storage||Desiccate at 4°C|
|Solubility||Limited solubility, soluble in DMSO or DMF|
|Chemical Name||2-(4-methyl-8-morpholin-4-ylsulfonyl-1,3-dioxopyrrolo[3,4-c]quinolin-2-yl)ethyl acetate|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|