526526

PIM3 Kinase Inhibitor VII, M-110

• Synonyme(s) : PIM3 Kinase Inhibitor VII, M-110, Nʹ-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide
• Formule empirique (notation de Hill): C₂₂H₂₈ClN₅O₃
• Poids moléculaire : 445.94
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.28

Propriétés

• Pureté: ≥97% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: pale yellow
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: wet ice
• Température de stockage: −20°C

Description

Description générale

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.

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; [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 at 5 µM). Shown to inhibit PIM3-dependent STAT3 Tyr705 phosphorylation in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells (by 73% and 83%, respectively; 10 µM for 18 h), while displaying little effect toward STAT3 Tyr694 phosphoylation in 22RV1 cultures.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable