FK-866A highly specific non-competitive inhibitor of NAMPT

FK-866 (CAS 658084-64-1)

FK-866 | CAS 658084-64-1 is rated 4.0 out of 5 by 1.
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Synonym: K 22.175; N-[4-(1-benzoyl-4-piperidinyl)butyl]-3-(3-pyridinyl)-2E-propenamide
Application: A highly specific non-competitive inhibitor of NAMPT
CAS Number: 658084-64-1
Purity: ≥98%
Molecular Weight: 391.5
Molecular Formula: C24H29N3O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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FK-866 has been shown to induce apoptosis by non-competitive, and specific inhibition of nicotamide phosphoribosyltransferase (NAMPT). NAMPT is a key regulatory enzyme that mediates NAD+ biosynthesis within cells. Mechanistic studies show that this compound contains an enzymatic active site of visfatin which is optimized for nicotinamide binding and inhibition. Visfatin also contains a similar structure to insulin and mimics its actions by binding to the insulin receptors.


References

. Hasmann, M. and Schemainda, I. 2003. Cancer Res. 63: 7436-7442. PMID: 14612543
2. Kim, M.K., et al. 2006. J. Mol. Biol. 362: 66-77. PMID: 16901503
3. van der Veer, E., et al. 2007. J. Biol. Chem. 282: 10841-10845. PMID: 17307730
4. Billington, R.A., et al. 2008. Autophagy. 4: 385-387. PMID: 18227641

Physical State :
Solid
Solubility :
Soluble in ethanol (78 mg/ml at 25° C), DMF (40 mg/ml), DMSO (100 mg/ml), PBS (pH 7.2) (~0.5 mg/ml), and water (<1 mg/ml at 25° C).
Storage :
Store at -20° C
Melting Point :
253.04° C (Predicted)
Boiling Point :
629.94° C at 760 mmHg (Predicted)
Density :
1.13 g/cm3 (Predicted)
Refractive Index :
n20D 1.59 (Predicted)
IC50 :
PBEF: IC50 = 0.09 nM; SH-SY5: IC50 = 0.5 nM (human); Delayed cell death by apoptosis: IC50 ~1 nM (Hep-G2 human liver carcinoma cells); MCF7: IC50 = 0.68 µM (human)
Ki Data :
NAMPT/NAPRT for the free enzyme: Ki= 0.3 nM; NAMPT/NAPRT for the enzyme/substrate complex: Ki= 0.4 nM
pK Values :
pKb: 4.24 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
6914657
MDL Number :
MFCD10565943
SMILES :
O=C(N1CCC(CCCCNC(/C=C/C2=CN=CC=C2)=O)CC1)C3=CC=CC=C3

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FK-866  Product Citations

See how others have used FK-866. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 26024774  Takeuchi, M. et al. 2015. Exp. Cell Res. 335: 62-7.

PMID: # 26542945  Zucal, C. et al. 2015. BMC Cancer. 15: 855.

PMID: # 24389478  Takeuchi, M. et al. 2014. Biol. Pharm. Bull. 37: 31-6.

PMID: # 23975935  Magnifico, S. et al. 2013. FASEB J. 27: 4712-22.

Citations 1 to 4 of 4 total
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Rated 4 out of 5 by from This has been working well in our research This has been working well in our research and we are going to publish soon.
Date published: 2015-09-10
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