Kenpaullone is an ATP-competitive inhibitor of several CDKs (cyclin-dependent kinases) as well as GSK-3β (glycogen synthase kinase 3β). It has been shown to inhibit GSK-3 with an IC50 value of 0.23 μM and CDK1/cyclin B, CDK2/cyclin A, CDK5/p25, and lymphocyte kinase with IC50 values of 0.4, 0.68, 0.85, and 0.47 μM, respectively. Due to the compound’s activity, Kenpaullone is useful in the study of cell cycle regulators. Kenpaullone is an inhibitor of cyclin E, ERK 2 and p35.