Nampt-IN-1

Nampt-IN-1 is a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt; IC₅₀ = 3.1 nM). It is selective for Nampt over a panel of greater than 100 human kinases at 1 μM. Nampt-IN-1 inhibits NAD⁺ formation in and proliferation of HCT116 cells (IC₅₀s = 1.8 and 8.9 nM, respectively). It inhibits cell growth in a panel of cancer cell lines (IC₅₀s = <0.2-2 μM). Nampt-IN-1 inhibits NAD⁺ formation in an A2780 ovarian carcinoma mouse xenograft model (ED₅₀ = 2 mg/kg).

Nampt-IN-1 functions as a co-drug. Nampt-IN-1 is a potent and selective NAMPT inhibitor.

LSN3154567 might be useful in developing a novel cancer therapeutic.