126871

Alsterpaullone, 2-Cyanoethyl - CAS 852529-97-0 - Calbiochem

A cell-permeable and reversible Alsterpaullone derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3β.

• Sinônimo(s): Alsterpaullone, 2-Cyanoethyl - CAS 852529-97-0 - Calbiochem, 3-(6-Oxo-9-nitro-5,6,7,12-tetrahydroindolo[3,2-d][1]benzazepin-2-yl)propionitrile
• Fórmula empírica (Notação de Hill): C₁₉H₁₄N₄O₃
• Número CAS: 852529-97-0
• Peso molecular: 346.34
• Código UNSPSC: 12352200

Propriedades

• Ensaio: ≥90% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: light orange
• solubilidade: DMSO: 10 mg/mL
• Condições de expedição: wet ice
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

A cell-permeable and reversible Alsterpaullone (Cat. No. 126870) derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdk1/cyclin B and GSK-3β (IC₅₀ = 230 pM and 800 pM, respectively; [ATP] = 15 µM). Displays ~37-fold greater selectivity for Cdk1/cyclin B over Cdk5/p25 (IC₅₀ = 30 nM). Shown to inhibit other kinases in a commercially available testing screen panel (pIC₅₀ = −logIC₅₀[M]; pIC₅₀ = ~ 7.5, 7.0, 7.0, 6.5, 6.5, 6.0, and 6.0 for Cdk2/A, Cdk4/D1, GSK-3β, PDGFRβ, Src, VEGFR-2, and VEGFR-3, respectively; [ATP] = 1 µM).

A cell-permeable and reversible Alsterpaullone (Cat. No. 126870) derivative that acts as a highly potent and ATP-competitiveinhibitor of Cdk/GSK-3 family serine/threonine kinases (IC₅₀ = 230 pM and 800 pM for cdk1/cyclin B and Gsk-3β, respectively; [ATP] = 15 µM). Displays ~130-fold greater selectivity for Cdk1/cyclin B over Cdk5/p25 (IC₅₀ = 30 nM). Shown to inhibit tyrosine kinases only at higher concentrations (pIC₅₀ = −logIC₅₀[M]; pIC₅₀ ~7.5, 7.0, 7.0, 6.5, 6.5, 6.0, and 6.0 for Cdk2/A, Cdk4/D1, GSK-3β, PDGFRβ, Src, VEGFR-2, and VEGFR-3, respectively; [ATP] = 1 µM).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
Cdkl/Gsk-3β, Cyclin B

Product competes with ATP.

Reversible: yes

Target IC₅₀: 230 pM and 800 pM, [ATP] = 15 µM, against Cdk1/cyclin B and GSK-3β, respectively

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Nota de preparo

Slight warming may be required for complete solubilization.

Reconstituição

Following reconstitution, aliquot and refrigerate (4°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Kunick, C., et al. 2005. ChemBioChem.6, 541.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 2
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable