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.

• Synonym(e): 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
• Empirische Formel (Hill-System): C₁₉H₁₄N₄O₃
• CAS-Nummer: 852529-97-0
• Molekulargewicht: 346.34
• UNSPSC-Code: 12352200

Eigenschaften

• Assay: ≥90% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: light orange
• Löslichkeit: DMSO: 10 mg/mL
• Versandbedingung: wet ice
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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).

Biochem./physiol. Wirkung

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

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Angaben zur Herstellung

Slight warming may be required for complete solubilization.

Rekonstituierung

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

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 2
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable