SMI-16a

Pim

-20

SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM).

A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive inhibitor against Pim-1/2 kinases (IC50 = 150 nM and 20 nM against Pim-1 and Pim-2, respectively) as well as DYRK1alpha (68% inhibition of DYRK1alpha and Pim-2 at 5 uM), while exhibiting little or no activity against a panel of 57 other kinases (<=18% inhibition at 5 uM). Reported to exhibit antitumor activity both in PC3 human prostate cancer cultures in vitro (IC50 = 48 uM) and in JC adenocarcinoma-transplanted Balb/C mice in vivo (ca.46% tumor mass reduction on day 20; 50 mg/kg via daily i.p.).