产品描述
GPP78 is a potent inhibitor of Nampt (IC50: 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion). GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells (IC50: 3.8 nM by inducing autophagy). GPP78 has anti-cancer and anti-inflammatory effects.
体外活性
GPP78 appears truly cytotoxic in melanoma cell lines, while in the others it is mainly cytostatic. GPP78 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 (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].
体内活性
GPP78 (i.p.; daily; 10 mg/kg; 1 hour or 6 hours after SCI; for 19 days; male adult CD1 mice) treatment decreases the severity of spinal cord trauma in SCI mice [2].
Cas No.
1202580-59-3
分子式
C27H29N5O
分子量
439.55
别名
CAY10618;GPP78
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years