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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

FK-866

Cayman Chemical Item Number 13287

K 22.175 (CAS 658084-64-1)

FK-866 (CAS 658084-64-1)

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Description

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., and 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).

Synonyms
  • K 22.175
Formal Name N-​[4-​(1-​benzoyl-​4-​piperidinyl)butyl]-​3-​(3-​pyridinyl)-​2E-​propenamide
CAS Number 658084-64-1
Molecular Formula C24H29N3O2
Formula Weight 391.5
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=C(N1CCC(CCCCNC(/C=C/C2=CN=CC=C2)​=O)​CC1)​C3=CC=CC=C3

Background Reading

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).

Hasmann, M., and 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).

Billington, R.A., Genazzani, A.A., Travelli, C., et al. NAD depletion by FK866 induces autophagy. Autophagy 4(3) 385-387 (2008).
Size Price Quantity Subtotal
5 mg $122.00 $0.00
10 mg $232.00 $0.00
25 mg $549.00 $0.00
50 mg $976.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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