Alsterpaullone

Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC₅₀s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC₅₀s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders^[1]. Alsterpaullone induces apoptosis in leukemia cell line^[2]. IC50 & Target: IC50: 35 nM (CDK1/cyclin B), 15 nM (CDK2/cyclin A), 200 nM (CDK2/cyclin E), 40 nM (CDK5/p35), 4 nM (GSK-3a/GSK-3beta)^[1] In Vitro: Alsterpaullone (0.3, 1, 3 μM; 8 hours) induces apoptosis in leukemia cell line^[2].
Alsterpaullone (5, 10, 15, 20, 25, 30 μM; 48 and 72 hours) inhibits the growth of HeLa cells in dose-and time-dependent manner. Treatment with Alsterpaullone causes a time-dependent inhibition of cell growth too^[3].
Alsterpaullone (20?μM) induces cell death depending on caspase activity^[3]. In Vivo: Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts^[4].