Date published: 2026-2-1

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FK-866 (CAS 658084-64-1)

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Alternate Names:
K 22.175; N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2E-propenamide
Application:
FK-866 is A highly specific non-competitive inhibitor of NAMPT
CAS Number:
658084-64-1
Purity:
≥98%
Molecular Weight:
391.5
Molecular Formula:
C24H29N3O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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FK-866 may act to induce apoptosis by non-competitive, and specific inhibition of PBEF (nicotamide phosphoribosyltransferase, NAMPT). PBEF (NAMPT) is a key regulatory enzyme that mediates NAD+ biosynthesis within cells. Mechanistic studies show that this compound contains an enzymatic active site of visfatin which is optimized for nicotinamide binding and inhibition. Visfatin also contains a similar structure to insulin and mimics its actions by binding to the insulin receptors.


FK-866 (CAS 658084-64-1) References

  1. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis.  |  Hasmann, M. and Schemainda, I. 2003. Cancer Res. 63: 7436-42. PMID: 14612543
  2. Antiangiogenic potency of FK866/K22.175, a new inhibitor of intracellular NAD biosynthesis, in murine renal cell carcinoma.  |  Drevs, J., et al. 2003. Anticancer Res. 23: 4853-8. PMID: 14981935
  3. Crystal structure of visfatin/pre-B cell colony-enhancing factor 1/nicotinamide phosphoribosyltransferase, free and in complex with the anti-cancer agent FK-866.  |  Kim, MK., et al. 2006. J Mol Biol. 362: 66-77. PMID: 16901503
  4. Extension of human cell lifespan by nicotinamide phosphoribosyltransferase.  |  van der Veer, E., et al. 2007. J Biol Chem. 282: 10841-5. PMID: 17307730
  5. NAD depletion by FK866 induces autophagy.  |  Billington, RA., et al. 2008. Autophagy. 4: 385-7. PMID: 18227641
  6. Nicotinamide mononucleotide adenylyltransferase 1 gene NMNAT1 regulates neuronal dendrite and axon morphogenesis in vitro.  |  Zhao, H., et al. 2011. Chin Med J (Engl). 124: 3373-7. PMID: 22088538
  7. Hepatectomy-related hypophosphatemia: a novel phosphaturic factor in the liver-kidney axis.  |  Nomura, K., et al. 2014. J Am Soc Nephrol. 25: 761-72. PMID: 24262791
  8. Nicotinamide phosphoribosyltransferase inhibitor is a novel therapeutic candidate in murine models of inflammatory lung injury.  |  Moreno-Vinasco, L., et al. 2014. Am J Respir Cell Mol Biol. 51: 223-8. PMID: 24588101
  9. NAMPT regulates mitochondria biogenesis via NAD metabolism and calcium binding proteins during skeletal muscle contraction.  |  Kim, JS., et al. 2014. J Exerc Nutrition Biochem. 18: 259-66. PMID: 25566462
  10. Nutritional energy stimulates NAD+ production to promote tankyrase-mediated PARsylation in insulinoma cells.  |  Zhong, L., et al. 2015. PLoS One. 10: e0122948. PMID: 25876076
  11. The sensitivity of adipose tissue visfatin mRNA expression to lipopolysaccharide-induced endotoxemia is increased by ovariectomy in female rats.  |  Iwasa, T., et al. 2016. Int Immunopharmacol. 35: 243-247. PMID: 27083000
  12. Nicotinamide Phosphoribosyltransferase Attenuates Methotrexate Response in Juvenile Idiopathic Arthritis and In Vitro.  |  Funk, RS., et al. 2016. Clin Transl Sci. 9: 149-57. PMID: 27166432
  13. Inhibitor of Nicotinamide Phosphoribosyltransferase Sensitizes Glioblastoma Cells to Temozolomide via Activating ROS/JNK Signaling Pathway.  |  Feng, J., et al. 2016. Biomed Res Int. 2016: 1450843. PMID: 28097126
  14. Targeted Delivery of Cytotoxic NAMPT Inhibitors Using Antibody-Drug Conjugates.  |  Neumann, CS., et al. 2018. Mol Cancer Ther. 17: 2633-2642. PMID: 30242091
  15. FK866 attenuates sepsis-induced acute lung injury through c-jun-N-terminal kinase (JNK)-dependent autophagy.  |  Zheng, Q., et al. 2020. Life Sci. 250: 117551. PMID: 32179075
  16. FK866 inhibits colorectal cancer metastasis by reducing NAD+ levels in cancer-associated fibroblasts.  |  Xie, H., et al. 2022. Genes Genomics. 44: 1531-1541. PMID: 36214983

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

FK-866, 5 mg

sc-205325
5 mg
$143.00

FK-866, 10 mg

sc-205325A
10 mg
$250.00