Kenpaullone

142273-20-9

C16H11BrN2O

DMSO : >= 35 mg/mL (106.97 mM)

Stem Cell/Wnt; PI3K/Akt/mTOR; Cell Cycle/DNA Damage

Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3beta, with IC₅₀s of 0.4 uM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC₅₀s of 0.68 uM, 7.5 uM, 0.85 uM, respectively. IC50 & Target: IC50: 0.4 uM (CDK1/cyclin B), 0.68 uM (CDK2/cyclin A), 7.5 uM (CDK2/cyclin E), 0.85 uM (CDK5/p25)^[1], 23 nM (GSK-3beta)^[2] In Vitro: Kenpaullone shows much less effect on c-src (IC₅₀, 15 uM), casein kinase 2 (IC₅₀, 20 uM), erk 1 (IC₅₀, 20 uM), and erk 2 (IC₅₀, 9 uM). Kenpaullone acts by competitive inhibition of ATP binding, and the apparent K_i is 2.5 uM. Kenpaullone can inhibit the growth of tumor cells in culture (mean GI₅₀, 43 uM) and causes altered cell cycle progression most clearly revealed under conditions of recovery from serum starvation^[1]. Kenpaullone demonstrates a wide range of biological utility, extending from maintenance of pancreatic beta cell survival and proliferation to the induction of apoptosis in cancer cells^[2].