Caspase Modulator I, 1541-Calbiochem

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一般描述

A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC₅₀= 35 and 38 ?M, respectively) by targeting both the large and small subunit active sites. Kinetic studies with 1541 and its 8-Hydroxy analog (Cat. No. 529663) indicate that at suboptimal inhibitor : proenzyme molar ratio (100:1 or less), the compound does not effectively occupies both active sites of and stabilizes the proenzyme in an “on-state” conformation that facilitates the subsequent autoproteolysis or autoactivation process via the unoccupied active site of procaspase-3 and -6 (EC₅₀= 2.4 and 2.8 ?M, respectively). Shown to effectively induce apoptosis (up to 50 ?M) in various cancer cell lines (IC₅₀ranges from 3.8 to 8.7 ?M) in a caspase-3-dependent, but p53-, caspase-8-, and Bak-independent manner. Exhibits little inhibitory effect against active caspase-7 (30 nM) even at concentrations as high as 50 ?M, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.
A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC₅₀= 35 and 38 ?M, respectively) by targeting both the large and small subunit active sites. Kinetic studies with 1541 and its 8-Hydroxy analog (Cat. No. 529663) indicate that at suboptimal inhibitor : proenzyme molar ratio (100:1 or less), the compound does not effectively occupies both active sites of and stabilizes the proenzyme in an “on-state” conformation that facilitates the subsequent autoproteolysis or autoactivation process via the unoccupied active site of procaspase-3 and -6 (EC₅₀= 2.4 and 2.8 ?M, respectively). Shown to effectively induce apoptosis (up to 50 ?M) in various cancer cell lines (IC₅₀ranges from 3.8 to 8.7 ?M) in a caspase-3-dependent, but p53-, caspase-8-, and Bak-independent manner. Exhibits little inhibitory effect against active caspase-7 (30 nM) even at concentrations as high as 50 ?M, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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