A potent Nampt inhibitor (IC50 = 3.1 nM); selective for Nampt over a panel of >100 human kinases at 1 μM; inhibits NAD+ formation in and proliferation of HCT116 cells (IC50s = 1.8 and 8.9 nM, respectively); inhibits cell growth in a panel of cancer cell lines (IC50s = + formation in an A2780 ovarian carcinoma mouse xenograft model (ED50 = 2 mg/kg)