Uses
Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of caspase-3.
Definition
ChEBI: Acetic acid 2-[4-methyl-8-(4-morpholinylsulfonyl)-1,3-dioxo-2-pyrrolo[3,4-c]quinolinyl]ethyl ester is a pyrroloquinoline.
General Description
A cell-permeable, non-peptidyl pyrroloquinoline compound that acts as a potent, reversible, and non-competitive inhibitor of caspase-3 (IC50 = 23 nM) with larger than 10-fold greater selectivity towards caspase-3 than caspases-1, -2, and -4 through -10. Shown to display higher anti-apoptotic activity than Z-VAD-FMK (Cat. No. 627610) in preventing Staurosporine- (Cat. No. 569397) induced apoptosis in human Jurkat T cells.
Biological Activity
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].
Biochem/physiol Actions
Cell permeable: yes
References
[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.
