Alsterpaullone, 2-Cyanoethyl

Alsterpaullone, 2-Cyanoethyl is an alsterpaullone derivative that acts as a highly potent, ATP-competitive, selective inhibitor of Cdc2 (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). In a commercially available testing screen panel, shows to inhibit other kinases (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).