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).

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

Packaged under inert gas

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

Slight warming may be required for complete solubilization.

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

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

Toxicity: Standard Handling (A)