481908

FK866 hydrochloride hydrate

The Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, also referenced under CAS 658084-64-1, controls the biological activity of Nicotinamide Phosphoribosyltransferase. This small molecule/inhibitor is primarily used for Neuroscience applications.

• 別名: Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, (E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor, APO866, NAMPTase Inhibitor I, PBEF Inhibitor I, Visfatin Inhibitor I, NAPRT Inhibitor, APO866, NAMPTase Inhibitor I, PBEF Inhibitor I, Visfatin Inhibitor I, NAPRT Inhibitor, (E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor
• 実験式（ヒル表記法）: C₂₄H₂₉N₃O₂
• CAS番号: 658084-64-1
• 分子量: 391.51
• MDL number: MFCD10565943
• UNSPSC Code: 51111800
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: liquid
• Storage condition: OK to freeze, protect from light

特性

• 製品名: Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, The Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, also referenced under CAS 658084-64-1, controls the biological activity of Nicotinamide Phosphoribosyltransferase. This small molecule/inhibitor is primarily used for Neuroscience applications.
• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: yellow
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: N2(CCC(CC2)CCCCNC(=O)\C=C\c3cnccc3)C(=O)c1ccccc1
• InChI: 1S/C24H29N3O2/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28)/b12-11+
• InChI key: KPBNHDGDUADAGP-VAWYXSNFSA-N

詳細

General description

A cell-permeable pyridinylacrylamide compound that acts as a selective, allosteric NAPRT/NAMPT (nicotinamide phosphoribosyltransferase) inhibitor (K_i = 0.4 nM for the enzyme/substrate complex; K_i^′ = 0.3 nM for the free enzyme), while exhibiting no effect toward NPRT (nicotinic acid phosphoribosyltransferase) activity (82% inhibition of NAPRT activity at 10 nM vs no inhibition of NPRT activity at 1 µM in K-562 extract). FK866 treatment is shown to induce cell death by depleting NAD⁺ (Cat. Nos. 481911 & 481915 ) in HepG2 and NIH-3T3 cultures (by >95% after 24 h treatment of 10 nM FK866), likewise the addition of exogenous NAD⁺ is demonstrated to rescue NIH-3T3 and SH-SY5Y from FK866-induced NAD⁺-depletion and cell death.

Packaging

Packaged under inert gas

Physical form

Supplied as a 50 mM (2 mg/102.17 µl) solution in DMSO.

Other Notes

Formentini, L., et al. 2009. Biochem. Pharmacol.77, 1612.
Nakahata, Y., et al. 2009. Science324, 654.
Ramsey. K.M., et al. 2009. Science324, 651.
Billington, R.A., et al. 2008. J. Biol. Chem.283, 6367.
Hasmann, M. and Schemainda, I., 2003. Cancer Res.63, 7436.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

安全性情報

• 保管分類: 11 - Combustible Solids
• 一体何が起きているの？: WGK 2
• 引火点 (F): Not applicable
• 引火点（°C）: Not applicable