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.
IC50&Target
Nampt;
Autophagy
体外研究
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.
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.
Western Blot Analysis
Cell Line:
SH-SY5Y cells
Concentration:
10 nM
Incubation Time:
24 hours, 40 hours
Result:
Punctate staining of LC3-II and the formation of autophagolysosomes were observable.
体内研究
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.
Animal Model:
Male adult CD1 mice (25-30 g) with spinal cord injury (SCI)
Dosage:
10 mg/kg
Administration:
Intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days
Result:
Significantly reduced the demyelination associated with SCI. And significantly ameliorated the functional deficits induced by SCI.
分子式
C27H29N5O
分子量
439.55
CAS号
1202580-59-3
运输条件
Room temperature in continental US; may vary elsewhere.