PIM1/2 Kinase Inhibitor V

A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive inhibitor against Pim-1/2 kinases (IC₅₀ = 24 nM and 100 nM against Pim-1 and Pim-2, respectively), while exhibiting little or no activity against a panel of 58 other kinases (≤20% inhibition at 5 µM). One h inhibitor treatment (0.5 µM) of HEK-293T cultures at the end of a 4 h ³²PO₄ incubation period results in nearly complete inhibition of the autophosphorylation of overexpressed Pim-1. Comparing to Inhibitor VI (Cat. No. 526524), Inhibitor V is less reactive towards DYRK1α (20% vs. 68% inhibition with respective inhibitor at 5 µM) and more potent in PC3 human prostate cancer cell killing (IC₅₀ = 17 vs. 48 µM with respective inhibitor).

A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive inhibitor against Pim-1/2 kinases (IC₅₀ = 24 nM and 100 nM against Pim-1 and Pim-2, respectively), while exhibiting little or no activity against a panel of 58 other kinases (≤20% inhibition at 5 µM). One hour inhibitor treatment (0.5 µM) of HEK-293T cultures at the end of a 4 hour ³²PO₄ incubation period results in nearly complete inhibition of the autophosphorylation of overexpressed Pim-1. Comparing to Inhibitor VI (Cat. No. 526524), Inhibitor V is less reactive towards DYRK1α (20% vs. 68% inhibition with respective inhibitor at 5 µM) and more potent in PC3 human prostate cancer cell killing (IC₅₀ = 17 vs. 48 µM with respective inhibitor).

Packaged under inert gas

Toxicity: Standard Handling (A)

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

Lin,Y., et al. 2009. Blood In press.
Xia, Z., et al. 2009. J. Med. Chem.52, 74.

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