CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively. It is for research use only and not sold to patients.
- Potent and kinase selective pan-Pim kinases inhibitor
- Inhibits Pim-1 with an IC50 of 5 nM, Pim-2 with an IC50 of 25 nM, and Pim-3 with an IC50 of 16 nM
- Causes dose-dependent inhibition of the phosphorylation of pro-survival proteins Bad and 4E-BP1 at specific Pim kinase sites (S112, S65, T37/46)
- Diminishes steady-state levels of ectopic NKX3.1 in PC3 cells and reduces NKX3.1 half-life
- Exhibits robust in vivo efficacy in two Pim kinases driven tumor models, with 50 mg/kg producing 45% tumor growth inhibition (TGI) and 100 mg/kg producing 75% TGI