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Cat. No. Name Size Price Add Cart
KI3525FK86610 mg$260

Chemical Characteristic

Product NameFK866
SynonymsAPO866
CAS No.658084-64-1
Molecular Weight 391.5
FormulaC24H29N3O2
Chemical Name(2E)-N-[4-(1-Benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamide
SmilesC(=O)(/C=C/c1cnccc1)NCCCCC1CCN(CC1)C(=O)c1ccccc1
Chemical Structure

Biological activities

FK866 is a highly specific noncompetitive inhibition of nicotinamide phosphoribosyltransferase (NAPRT). FK866 effectively induces delayed cell death by apoptosis in HepG2 human liver carcinoma cells with an IC50 of 1 nM. FK866 inhibits enzyme NAPRT/substrate complex and the free enzyme NAPRT with Ki values of 0.4 and 0.3 nM, respectively. In the cytoplasmic extracts from both cell lines, HepG2 and K-562, addition of 10 nM FK866 effectively inhibits NAM formation from nicotinamide. FK866 inhibits cellular NAD+ biosynthesis from the precursor nicotinamide with high specificity.[1] In SH-SY5Y neuroblastoma cells, after 72 hours of treatment, FK866 displays an IC50 of 0.93 nM. FK866 causes a concentration-dependent reduction in intracellular NAD(P) levels consistent with the cell count and MTT data when measured after 24 hours of treatment.[2] FK866 suppresses gastric cancer BGC823 cells migration and anchorage-independent growth. FK866 also increases the chemo-sensitivity of gastric cancer BGC823 cells to fluorouracil by inhibition of cell proliferation and the induction of apoptosis. FK866 reduces the expression of VEGF, matrix metalloproteinase 2 (MMP2), MMP9 and NF-ΚB in gastric cancer cells.[3] Treatment of mice with FK866 significantly ameliorates the functional deficits induced by spinal cord injury (SCI). FK866 modulates cytokines expression and neutrophil infiltration after SCI.[4]

Protocols

In vivo, FK866 is dissolved in non-pyrogenic saline.[4]

References

[1] Hasmann M, et al. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis. Cancer Res. 2003, 63(21): 7436-7442.
[2] Billington RA, et al. NAD depletion by FK866 induces autophagy. Autophagy. 2008, 4(3): 385-387.
[3] Bi TQ, et al. Overexpression of Nampt in gastric cancer and chemopotentiating effects of the Nampt inhibitor FK866 in combination with fluorouracil. Oncol Rep. 2011, 26(5): 1251-1257.
[4] Esposito E, et al. The NAMPT inhibitor FK866 reverts the damage in spinal cord injury. J Neuroinflammation. 2012, 9: 66.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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