Cell-permeable. FK-866 is a highly specific non-competitive inhibitor of Nicotinamide phosphoribosyltransferase (NAMPT) (Ki = 0.4 nM), causing gradual NAD+ depletion. NAMPT functions as an intra-cellular and extra-cellular NAD biosynthetic enzyme that is important for regulating metabolism and stress resistance through sirtuins and other NAD-consuming regulators. NAD+ depletion by FK-866 directs delayed cell death by apoptosis in Hep-G2 human liver carcinoma cells (IC50 = ~1 nM).
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A highly specific non-competitive inhibitor of Nicotinamide phosphoribosyltransferase (NAMPT)
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