FK-866

For research use only. Not for therapeutic Use.

  • CAT Number: I004482
  • CAS Number: 658084-64-1
  • Molecular Formula: C₂₄H₂₉N₃O₂
  • Molecular Weight: 391.51
  • Purity: ≥95%
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FK-866(Cat No.:I004482)is a highly potent inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), a key enzyme in the NAD+ biosynthesis pathway. By depleting cellular NAD+ levels, FK-866 disrupts energy metabolism and induces apoptosis, particularly in rapidly proliferating cancer cells. It has been studied extensively for its potential in cancer therapy, especially in tumors with high metabolic demands. FK-866’s mechanism of action also makes it a valuable tool for studying metabolic pathways and cell death processes, providing insight into novel therapeutic approaches for cancer treatment.


Catalog Number I004482
CAS Number 658084-64-1
Synonyms

(E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide

Molecular Formula C₂₄H₂₉N₃O₂
Purity ≥95%
Target Transferase
Solubility DMSO: 25 mg/mL
Storage 3 years -20C powder
IC50 0.09 nM
IUPAC Name (E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-pyridin-3-ylprop-2-enamide
InChI 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+
InChIKey KPBNHDGDUADAGP-VAWYXSNFSA-N
SMILES C1CN(CCC1CCCCNC(=O)/C=C/C2=CN=CC=C2)C(=O)C3=CC=CC=C3
Reference

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<br>[1]. Cea M, Cagnetta A, Fulciniti M, et al . Targeting NAD+ salvage pathway induces autophagy in multiple myeloma cells via mTORC1 and extracellular signal-regulated kinase (ERK1/2) inhibition. Blood. 2012 Oct 25;120(17):3519-29.
<br>[2]. Magnone M, Bauer I, Poggi A, et al. NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes. J Biol Chem. 2012 Jun 15;287(25):21067-81.
<br>[3]. Nin V, Escande C, Chini CC,et al. Role of deleted in breast cancer 1 (DBC1) protein in SIRT1 deacetylase activation induced by protein kinase A and AMP-activated protein kinase. J Biol Chem. 2012 Jul 6;287(28):23489-501.
<br>[4]. Thakur BK, Dittrich T, Chandra P, et al. Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells. Biochem Biophys Res Commun. 2012 Aug 3;424(3):371-7.
<br>[5]. Aimable Nahimana, Antoine Attinger, Dominique Aubry, et al. The NAD biosynthesis inhibitor APO866 has potent antitumor activity against hematologic malignancies. Blood April 2, 2009 ,113 (14): 3276-3286
<br>[6]. Mun-Kyoung Kim, Jun Hyuck Lee, Hun Kim, et al. Crystal Structure of Visfatin/Pre-B Cell Colony-enhancing Factor 1/Nicotinamide Phosphoribosyltransferase, Free and in Complex with the Anti-cancer Agent FK-866. Journal of Molecular Biology. 2006,362(1):66-77
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