The development of selective, cell-permeable protein kinase inhibitors for the treatment of cancer, inflammation, and other diseases, is a major focus of drug development efforts. Kenpaullone is an ATP-competitive inhibitor of several cyclin-dependent kinases (CDKs) as well as glycogen synthase kinase 3β (GSK-3β).1,2,3 It inhibits GSK-3β with an IC50 value of 0.023 µM3 (0.23 µM)2 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.1
1
Zaharevitz, D.W., Gussio, R., Leost, M., et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res592566-2569(1999).
2
Bain, J., McLauchlan, H., Elliot, M., et al. The specificities of protein kinase inhibitors: An update. Biochem J371199-204(2003).
3
LeClerc, S., Garnier, M., Hoessel, R., et al. Indirubins inhibit glycogen synthase kinase-3β and CDK5/P25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors?J Biol Chem276(1)251-260(2001).
Zaharevitz, D.W., Gussio, R., Leost, M., et al. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res592566-2569(1999).
Bain, J., McLauchlan, H., Elliot, M., et al. The specificities of protein kinase inhibitors: An update. Biochem J371199-204(2003).
LeClerc, S., Garnier, M., Hoessel, R., et al. Indirubins inhibit glycogen synthase kinase-3β and CDK5/P25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors?J Biol Chem276(1)251-260(2001).
Kenpaullone is available in the following screening
library: