PIM3 Kinase Inhibitor VII, M-110

A cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (K_i = 0.3 µM), and highly isoform-selective PIM inhibitor (IC₅₀ = 2.5, 2.5, and 0.047 µM against PIM1, PIM2, and PIM3, respectively, with PIMtide as substrate, [ATP] = 10 µM), while affecting CK2α2 only at much higher concentrations (IC₅₀ = 5 µM, [ATP] = 10 µM) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition; [M-110] = 5 µM). M-100 treatment (10 µM for 18 hr) is shown to inhibit both basal (by 73% and 83% of DMSO control in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells, respectively) and IL-6-stimulated (by 69% of DMSO control in DU-145 cells) STAT3 phosphorylation on Tyr705, while displaying little effect toward Tyr694 phosphoylation (in 22RV1 cultures). Isoform-specific knockdowns in DU-145 cells likewise identify PIM-3, but not PIM-1 or -2, as the kinase responsible for cellular STAT3 Tyr705 phosphorylation.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 months at -20°C.

Chang, M., et al. 2010. Mol. Cancer Ther.9, 2478.

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

Toxicity: Standard Handling (A)