GPP78

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]. IC50 & Target: Nampt^[1];
Autophagy^[1] 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].