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Nampt-IN-1 is a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt; IC50 = 3.1 nM).1 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).
WARNING This product is not for human or veterinary use.
1. Discovery of a highly selective NAMPT inhibitor that demonstrates robust efficacy and improved retinal toxicity with nicotinic acid coadministration. Mol. Cancer Ther. 16(12), 2677-2688 (2017).