MilliporeSigma™ Calbiochem™ Caspase Modulator I, 1541

Description

A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC₅₀ = 35 and 38μM, respectively) by targeting both the large and small subunit active si

A cell-permeable phenylimidazopyridinyl-methoxy coumarin compound that inhibits caspase-3 and caspase-6 activities (IC₅₀ = 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 (EC₅₀ = 2.4 and 2.8μM, respectively). Shown to effectively induce apoptosis (up to 50μM) in various cancer cell lines (IC₅₀ 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.

Specifications

• Color: Yellow
• Description: 95% by HPLC
• Molecular Formula: C₂₄H₁₇N₃O₄
• Formula Weight: 411.4g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Solid
• Quantity: 10 mg