GPP78

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GPP78

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1202580-59-3
包装:	5mg (11.38 mM * 1 mL in Methanol)
市场价:	5400元

产品名称

CAY10618

产品介绍

GPP78 (CAY10618) 是一种有效的烟酰胺磷酸核糖转移酶 (Nampt) 抑制剂，对NAD消耗的IC₅₀为 3 nM。GPP78 通过诱导自噬对神经母细胞瘤细胞 SH-SY5Y 具有毒性，IC₅₀为 3.8 nM。GPP78 具有抗癌和抗炎作用。

生物活性

GPP78 (CAY10618) is a potentNamptinhibitor with anIC₅₀of 3.0 nM fornicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with anIC₅₀of 3.8 nM by inducingautophagy. GPP78 has anti-cancer and anti-inflammatory effects^[1]^[2].

IC₅₀& Target

Nampt^[1];
Autophagy^[1]

体外研究
(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].

Western Blot Analysis^[1]

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
(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].

Animal Model:	Male adult CD1 mice (25-30 g) with spinal cord injury (SCI)^[2]
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.

分子量

439.55

性状

Liquid

Formula

C₂₇H₂₉N₅O

CAS 号

1202580-59-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Solution, -20°C, 2 years