Caspase Modulator I; 1541

Code: 264157-10MG D2-231

General description

A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC50 = 35 and 38 µM, ...


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€236.10 10MG
€290.40 inc. VAT

General description

A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC50 = 35 and 38 µM, 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 µM, respectively). Shown to effectively induce apoptosis (up to 50 µM) in various cancer cell lines (IC50 ranges from 3.8 to 8.7 µM) 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 µM, 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 µM, 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 µM, respectively). Shown to effectively induce apoptosis (up to 50 µM) in various cancer cell lines (IC50 ranges from 3.8 to 8.7 µM) 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 µM, nor does it activate procaspase-1 or -7 even after prolonged incubations upto 4 and 24 h, respectively.

Legal Information

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

assay≥95% (HPLC)
coloryellow
formsolid
manufacturer/tradenameCalbiochem®
Quality Level100
shipped inambient
solubilityDMSO: 5 mg/mL
storage conditionprotect from light, OK to freeze
storage temp.2-8°C
Cas Number1100353-03-4
This product has met the following criteria to qualify for the following awards:



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