FK 866 hydrochloride

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Cat.No. 4808 - FK 866 hydrochloride | C24H29N3O2.HCl
Description: Non-competitive and potent NAMPT inhibitor; induces apoptosis and autophagy
Chemical Name: 2-(E)-N-[4-(1-Benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2-propenamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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Keywords: FK866 hydrochloride Nicotinamide phosphoribosyltransferase NMPRTase inhibitors inhibits autophagy apoptosis NAD NAMPT visfatin PBEF NAMPT

Citations for FK 866 hydrochloride

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
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Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Pathways for FK 866 hydrochloride

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