MilliporeSigma™ Calbiochem™ Caspase Modulator I, 1541

Description

• A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC 50 = 35 and 38μM, 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 (EC 50 = 2.4 and 2.8μM, respectively)
• Shown to effectively induce apoptosis (up to 50μM) in various cancer cell lines (IC 50 ranges from 3.8 to 8.7μM) in a caspase-3-dependent, but p53-, caspase-8-, and Bak-independent manner
• Exhibits little inhibitory effect against active caspase-7 (30nM) even at concentrations as high as 50μM, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.