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Submit ReviewFK 866 hydrochloride
Description: Potent and non-competitive 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)
Biological Activity for FK 866 hydrochloride
FK 866 hydrochloride is a non-competitive and potent inhibitor of NAMPT (nicotinamide phosphoribosyltransferase, 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 for FK 866 hydrochloride
| M. Wt | 427.97 |
| Formula | C24H29N3O2.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2727965-45-7 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for FK 866 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 2.14 | 5 with gentle warming | |
| DMSO | 42.8 | 100 |
Preparing Stock Solutions for FK 866 hydrochloride
The following data is based on the product molecular weight 427.97. Batch specific molecular weights may vary from batch to batch due to the degree 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 for FK 866 hydrochloride
References for FK 866 hydrochloride
References are publications that support the biological activity of the product.
Travelli et al (2011) Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etop. or cisp. 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
If you know of a relevant reference for FK 866 hydrochloride, please let us know.
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Keywords: FK 866 hydrochloride, FK 866 hydrochloride supplier, FK866, hydrochloride, Nicotinamide, phosphoribosyltransferase, NMPRTase, inhibitors, inhibits, autophagy, apoptosis, NAD, NAMPT, visfatin, PBEF, Apoptosis, Inducers, Autophagy, 4808, Tocris Bioscience
2 Citations for FK 866 hydrochloride
Citations are publications that use Tocris products. Selected citations for FK 866 hydrochloride include:
Ian A et al (2021) Upregulation of Antioxidant Capacity and Nucleotide Precursor Availability Suffices for Oncogenic Transformation. Cell Metab 33 94-109.e8 PMID: 33159852
Singh et al (2018) Nicotinamide Phosphoribosyltransferase Deficiency Potentiates the Antiproliferative Activity of MTX through Enhanced Depletion of Intracellular ATP. J Pharmacol Exp Ther 365 96 PMID: 29420256
Do you know of a great paper that uses FK 866 hydrochloride from Tocris? Please let us know.
Reviews for FK 866 hydrochloride
Average Rating: 5 (Based on 1 Review.)
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Filter by:
NAD inhibitor.
By
Kishor Pant on 04/07/2022
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Cancer and liver cell lines
FK866 Inhibits NAD+ production and NAMPT activity in cancer cells.
Inhibition of NAD in cancer cells requires 3-4 days of treatment
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