Caspase Modulator I, 1541 – Calbiochem

Descrição detalhada : A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC50 = 35 and 38 microM, 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 microM, respectively). Shown to effectively induce apoptosis (up to 50 microM) in various cancer cell lines (IC50 ranges from 3.8 to 8.7 microM) 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 microM, 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 microM, 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 microM, respectively). Shown to effectively induce apoptosis (up to 50 microM) in various cancer cell lines (IC50 ranges from 3.8 to 8.7 microM) 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 microM, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.
Sinónimos : Caspase Modulator I, 1541 - Calbiochem; Caspase-6 Inhibitor XI, Procaspase-3 Activator II, Procaspase-6 Activator I, 8-Methoxy-2-oxo-2H-chromene-3-carboxylic acid-(3-imidazo[1,2-a]pyridin-2-yl-phenyl)-amide, Caspase-3 Inhibitor XV
Fórmula molecula r: C24H17N3O4
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X10MG