PIM Kinase Inhibitor VIII, R8-T198wt - Calbiochem

General Description

The human p27^Kip1 C-terminus PIM-1 phosphorylation site- (Thr¹⁹⁸) containing sequence is synthesized with an N-terminal Arg octamer/R8-containing sequence to facilitate its use as a cell-permeable, substrate-competitive PIM-1 inhibitor. Reported to completely prevents human prostate carcinoma DU145-derived tumor expansion for up to 17 days (0.5 μmol/animal on days 0 & 5; intratumoral injection) in mice in vivo when combined with a single Taxol (Cat. No. 580555) dosage on day zero (60 mg/kg; i.p.). Studies using FITC-conjugated R8-T198wt demonstrate that R8-T198wt-induced cell cycle arrest and apoptosis in PIM-1-expressing DU145 cells are direct consequences of inhibition of PIM-1-mediated p27^Kip1 Thr¹⁹⁸ and Bad Ser¹¹² phosphorylation, respectively.