A cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (Ki = 0.3uM), and highly isoform-selective PIM inhibitor (IC50 = 2.5, 2.5, and 0.047uM against PIM1, PIM2, and PIM3, respectively; [ATP] = 10uM), while affecting CK2alpha2 only at much higher concentrations (IC50 = 5uM, [ATP] = 10uM) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition at 5uM). Shown to inhibit PIM3-dependent STAT3 Tyr705 phosphorylation in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells (by 73% and 83%, respectively; 10uM for 18h), while displaying little effect toward STAT3 Tyr694 phosphoylation in 22RV1 cultures.
Formula:C22H28ClN5O3
Solubility:DMSO
Molar Mass:445.9
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months after receipt at -20°C. Reconstitute with sterile buffer or ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
