MedChemExpress - Model GPP78 - 1202580-59-3

FromMedChemExpress LLC (MCE)

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].

GPP78

MCE China：GPP78

Brand：MedChemExpress (MCE)

Cat. No.HY-14374

CAS：1202580-59-3

Synonyms：CAY10618

Purity：99.0%

Storage：Solution, -20°C, 2 years

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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].

In Vivo：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].

IC50 & Target：Nampt[1]; Autophagy[1] Cellular Effect Cell Line Type Value Description References

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. [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]

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