264157

Caspase Modulator I, 1541

• Synonym(e): Caspase Modulator I, 1541, 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
• Empirische Formel (Hill-System): C₂₄H₁₇N₃O₄
• Molekulargewicht: 411.41
• UNSPSC-Code: 12352200
• NACRES: NA.54

Eigenschaften

• Assay: ≥95% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: yellow
• Löslichkeit: DMSO: 5 mg/mL
• Versandbedingung: ambient
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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.

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable