Identification | Back Directory | [Name]
IVACHTIN | [CAS]
745046-84-8 | [Synonyms]
IVACHTIN 2-(4-methyl-8-morpholin-4-ylsulfonyl-1,3-dioxopyrrolo[3,4-c]quinolin-2-yl)ethyl acetate 2-[4-Methyl-8-(morpholin-4-ylsulfonyl)-1,3-dioxo-1,3-dihydro-2H-pyrrolo[3,4-c]quinolin-2-yl]ethylacetate | [Molecular Formula]
C20H21N3O7S | [MDL Number]
MFCD09971108 | [MOL File]
745046-84-8.mol | [Molecular Weight]
447.46 |
Hazard Information | Back Directory | [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. |
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