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.
1. Zaharevitz, D W., et al., 1999. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer research. 59(11): 2566-9. PMID: 10363974 2. Leclerc, S., et al., 2001. Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer's disease. A property common to most cyclin-dependent kinase inhibitors? The Journal of biological chemistry. 276(1): 251-60. PMID: 11013232 3. Bain, Jenny., et al., 2003. The specificities of protein kinase inhibitors: an update. The Biochemical journal. 371(Pt 1): 199-204. PMID: 12534346
Brown to yellow powder
Soluble in DMSO (>25 mg/ml), ethyl acetate, DMSO:PBS(pH7.2)(1:1), and DMF. Insoluble in ethanol, and water.
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PlantePlante, et. al. (PubMed ID 16162845) found that by treating MH1C1 cells with kenpaullone, a GSK inhibitor, at 5 M or 10 M concentrations, there was a marked increase in the inactive form of GSK3 (compared to controls). This suggests that kenpaullone inhibits GSK3 in the cell line tested. -SCBT Publication Review
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