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 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| PubChem ID | 78243733 |
| InChI Key | MULSIBUGDPOSHV-CALJPSDSSA-N |
| Smiles | O=C(C2=CC=CC=C2)N1CCC(CCCCNC(/C=C/C3=CN=CC=C3)=O)CC1.Cl |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.8 | 100 | |
| water | 2.14 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 427.97. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.34 mL | 11.68 mL | 23.37 mL |
| 5 mM | 0.47 mL | 2.34 mL | 4.67 mL |
| 10 mM | 0.23 mL | 1.17 mL | 2.34 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Travelli et al (2011) Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etoposide or cisplatin in neuroblastoma cells. J.Pharmacol.Exp.Ther. 338 829 PMID: 21685314
Hasmann et al (2003) FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis. Cancer Res. 63 7436 PMID: 14612543
Galli et al (2008) Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage. ChemMedChem 3 771 PMID: 18247435
Keywords: FK 866 hydrochloride, supplier, FK866, hydrochloride, Nicotinamide, phosphoribosyltransferase, NMPRTase, inhibitors, inhibits, autophagy, apoptosis, NAD, NAMPT, visfatin, PBEF, Apoptosis, Inducers, Autophagy, NAMPT, NAMPT, Tocris Bioscience
