PIM1/2 Kinase Inhibitor VI

General description

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 DYRK1A (68% inhibition of DYRK1A and Pim-2 at 5 µM), while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 µM). Reported to exhibit antitumor activity both in PC3 human prostate cancer cultures in vitro (IC₅₀ = 48 µM) and in JC adenocarcinoma-transplanted Balb/C mice in vivo (~46% tumor mass reduction on day 20; 50 mg/kg via daily i.p.).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Xia, Z., et al. 2009. J. Med. Chem.52, 74.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Standard Handling (A)