SMI-16a is a Pim-1 kinase inhibitor (IC50 = 63 nM). It is selective for Pim-1 over a panel of 60 kinases. SMI-16a (5 μM) inhibits phosphorylation of the Pim-1 target protein Bad in DU145-Pim cells and inhibits the growth of PC3, DU145, LNCaP, K562, and MV4-11 cancer cells. It induces apoptosis and cell cycle arrest at the G1 phase in DU145 cells.