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).

Pim1:150 nM, Pim2:20 nM

PIM1/2 Kinase Inhibitor VI exhibits antitumor activity in PC3 human prostate cancer cultures in vitro (IC50: 48 μM).

PIM1/2 Kinase Inhibitor VI exhibits antitumor activity in JC adenocarcinoma-transplanted Balb/C mice in vivo (~46% tumor mass reduction on day 20; 50 mg/kg/day, i.p.).

Competition binding reactions used 25 μg human M1 CHO membrane protein, BQCA or vehicle, and 0.15 nM [3H]NMS in 96-well deep-well plates. Binding reactions (30 °C for 2-3 h) are terminated by rapid filtration. Nonspecific binding is determined by adding 10 μM atropine. Filter plates are ished 4×with ice-cold 20 mM HEPES, 100 mM NaCl, and 5 mM MgCl2, pH 7.4 using a 96-well harvester. Plates are dried and radioactivity counted with a microplate scintillation counter[1].