Cyclin-dependent kinases (Cdks) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Cdk1/5 Inhibitor is a pyrazolo [3,4-b] quioxaline that inhibits Cdk1/cyclin B and Cdk5/p25 (IC50s = 600 and 400 nM, respectively). It less potently inhibits GSK3β (IC50 = 1 μM) and does not block Cdc25 activity. This compound is used to help define the roles of Cdk1 and Cdk5 in various signaling pathways.