Ivachtin is a potent inhibitor of caspase-3 with IC50 value of 23 nM [1].

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 [1].

Reference:

[1]. 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.

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