Catalog Number: 4808
Chemical Name: 2-(E)-N-[4-(1-Benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamide hydrochloride
Biological Activity
Non-competitive and potent inhibitor of NAMPT (nicotinamide phosphoribosyltransferase, visfatin, PBEF1) (Ki = 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
  • M.Wt:
    427.97
  • Formula:
    C24H29N3O2.HCl
  • Solubility:
    Soluble to 5 mM in water with gentle warming and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etoposide or cisplatin in neuroblastoma cells.
    Travelli et al.
    J.Pharmacol.Exp.Ther., 2011;338:829
  2. 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
  3. Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage.
    Galli et al.
    ChemMedChem, 2008;3:771

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