FK 866

Biological Activity

FK 866 is a non-competitive and high-affinity inhibitor of NAMPT (nicotinamide phosphoribosyltransferase, PBEF1) (K_i = 0.3 nM); inhibits NAD biosynthesis. Induces delayed cell death by apoptosis in HepG2 human liver carcinoma cells (IC₅₀ ~1 nM). Induces apoptosis in four different neuroblastoma cell lines; also induces autophagy in SH-SY5Y cells. Potentiates the cytotoxic effects induced by Etoposide (Cat. No. 1226) and Cisplatin (Cat. No. 2251).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis.
   Hasmann et al.
   Cancer Res., 2003;63:7436
2. Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage.
   Galli et al.
   ChemMedChem, 2008;3:771
3. Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etop. or cisp. in neuroblastoma cells.
   Travelli et al.
   J.Pharmacol.Exp.Ther., 2011;338:829

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