GPP78  (Synonyms: CAY10618)

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].

Nampt^[1];
Autophagy^[1]

GPP78 (Compound 8; 10 nM; 24-40 hours; SH-SY5Y cells) treatment with cells, punctate staining of LC3-II and the formation of autophagolysosomes are observable. LC3-II is membrane-bound and is present in autophagosomes^[1].
GPP78 (Compound 8) inhibits the growth of most cell lines tested, with nanomolar potency (GI₅₀) in cell lines derived from leukemia, lung, CNS, colon, melanoma, ovarian, renal, and prostate cancers. GPP78 appears truly cytotoxic in melanoma cell lines, while in the others it is mainly cytostatic^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GPP78 (10 mg/kg; intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days; male adult CD1 mice) treatment reduces the severity of spinal cord trauma in SCI mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

439.55

C₂₇H₂₉N₅O

1202580-59-3

Liquid

Colorless to light yellow

O=C(CCCCCCCN1N=NC(C2=CN=CC=C2)=C1)NC3=CC=CC=C3C4=CC=CC=C4

Room temperature in continental US; may vary elsewhere.

Solution, -20°C, 2 years

• [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.  [Content Brief]

  [2]. Esposito E, et al. The NAMPT inhibitor FK866 reverts the damage in spinal cord injury. J Neuroinflammation. 2012 Apr 10;9:66.  [Content Brief]