smi-16a

Description: SMI-16a (Pim1/2 Inhibitor IV) is a novel, potent, selective, cell-permeable, ATP-competitive Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 uM for Pim1, Pim2 and PC3 cells, respectively. The Pim protein kinases are frequently overexpressed in prostate cancer and certain forms of leukemia and lymphoma. SMI-16a was identified by screening to be a Pim-1 inhibitor and was found to attenuate the autophosphorylation of tagged Pim-1 in intact cells. Although SMI-16a is a competitive inhibitor with respect to ATP, a screen of approximately 50 diverse protein kinases demonstrated that it has high selectivity for Pim kinases. SMI-16a demonstrated selectivities of more than 2500-fold and 400-fold for Pim-1 or Pim-2, respectively. Overall, SMI-16a has the potential to be developed into a novel anticancer agent.

References: J Med Chem. 2009 Jan 8; 52(1):74-86; Leukemia. 2015 Jan; 29(1):207-17.