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Beschreibung

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 DYRK1&alpha, (68% inhibition of DYRK1&alpha, and Pim-2 at 5 microM), while exhibiting little or no activity against a panel of 57 other kinases (&le,18% inhibition at 5 microM). Reported to exhibit antitumor activity both in PC3 human prostate cancer cultures in vitro (IC50 = 48 microM) and in JC adenocarcinoma-transplanted Balb/C mice in vivo (~46% tumor mass reduction on day 20, 50 mg/kg via daily i.p.).