PIM3 Kinase Inhibitor VII, M-110 (N’-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide)

Size

£531.00

SKU:: 217664
Molecular Weight:: 445.9
Purity:: ≥97% (HPLC)
Storage Conditions:: -20°C
Supplier:: United States Biological
Format:: Supplied as a pale yellow solid.
Extra Details:: 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.