13287  FK-866

K 22.175 (CAS 658084-64-1)

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• See more Inhibitors; Apoptosis; Cancer; Obesity

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Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the condensation of nicotinamide with 5-phosphoribosyl-1-pyrophosphate to yield nicotinamide mononucleotide, an intermediate step in the biosynthesis of nicotinamide adenine dinucleotide (NAD+). FK-866 is a highly specific non-competitive inhibitor of NAMPT (Ki = 0.4 nM), causing gradual NAD+ depletion.1 In Hep-G2 human liver carcinoma cells, NAD+ depletion by FK-866 directs delayed cell death by apoptosis (IC50 = ~1 nM).1 In normal human smooth muscle cells, FK-866 causes premature senescence, an effect that may be linked to decreased activity of the NAD+-dependent enzyme SIRT1.2 Also, FK-866 induces autophagy in SH-SY5Y neuroblastoma cells, as indicated by the formation of LC3-positive vesicles.3
1  Hasmann, M., Schemainda, I. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis. Cancer Res 63 7436-7442 (2003).
2  van der Veer, E., Ho, C., O'Neil, C., et al. Extension of human cell lifespan by nicotinamide phosphoribosyltransferase. J Biol Chem 282(15) 10841-10845 (2007).
3  Billington, R.A., Genazzani, A.A., Travelli, C., et al. NAD depletion by FK866 induces autophagy. Autophagy 4(3) 385-387 (2008).


Purchase 13287 FK-866

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This product is also available to buy in bulk quantities. Please contact our Sales Department for a quote or to purchase.

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Warning This product is not for human or veterinary use.

Pricing updated 2010-03-16.
Prices are subject to change without notice.

Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.

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