Inhibitor of nicotinamide phosphoribosyltransferase
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FK-866

Item No. 13287

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2E-propenamide
CAS Number
658084-64-1
Synonyms
  • APO-866
  • Daporinad
  • K 22.175
Molecular Formula
C24H29N3O2
Formula Weight
391.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 40 mg/mlDMSO: 25 mg/mlEthanol: 50 mg/mlEthanol:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
257 nm
SMILES
O=C(N1CCC(CCCCNC(/C=C/C2=CN=CC=C2)=O)CC1)C3=CC=CC=C3
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    FK-866 is a highly specific non-competitive inhibitor of Nampt (Ki = 0.4 nM), causing gradual NAD+ depletion.1 In HepG2 human liver carcinoma cells, NAD+ depletion by FK-866 directs delayed cell death by apoptosis (IC50 = ~1 nM).1 In normal human smooth muscle cells, FK-866 causes premature senescence, an effect that may be linked to decreased activity of the NAD+-dependent enzyme SIRT1.2 Also, FK-866 induces autophagy in SH-SY5Y neuroblastoma cells, as indicated by the formation of LC3-positive vesicles.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hasmann, M., and Schemainda, I. FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis. Cancer Res. 63(21), 7436-7442 (2003).

    2. van der Veer, E., Ho, C., O'Neil, C., et al. Extension of human cell lifespan by nicotinamide phosphoribosyltransferase. The Journal of Biological Chemisty 282(15), 10841-10845 (2007).

    3. Billington, R.A., Genazzani, A.A., Travelli, C., et al. NAD depletion by FK866 induces autophagy. Autophagy 4(3), 385-387 (2008).

    Product Citations

    Ting, K.K.Y., Ibrahim, H.M., Gulati, N., et al. Intracellular accumulation of free cholesterol in macrophages triggers a PARP1 response to DNA damage and PARP1 impairs lipopolysaccharide-induced inflammatory response. PLoS One 20(3), e0318267 (2025).

    Kremer, D.M., Nelson, B.S., Lin, L., et al. GOT1 inhibition primes pancreatic cancer for ferroptosis through the autophagic release of labile iron. bioRxiv (2020).

    Huang, P., Lee, M.W.J., Sadrerafi, K., et al. MC-PPEA as a new and more potent inhibitor of CLP-induced sepsis and pulmonary inflammation than FK866. Drug Des. Devel. Ther. 11, 629-641 (2017).