Description

Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD⁺ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD⁺ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC₅₀ = 3 nM). It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC₅₀ value of 3.8 nM through a process that appears to involve autophagy.

Uses

GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects[1][2].

Definition

ChEBI: N-(2-phenylphenyl)-8-[4-(3-pyridinyl)-1-triazolyl]octanamide is a member of biphenyls.

in vivo

References

[1] Colombano G, et al. A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistry. J Med Chem. 2010 Jan 28;53(2):616-23. DOI:10.1021/jm9010669
[2] Esposito E, et al. The NAMPT inhibitor FK866 reverts the damage in spinal cord injury. J Neuroinflammation. 2012 Apr 10;9:66. DOI:10.1186/1742-2094-9-66