GPP78(Synonyms: CAY10618)

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GPP78 (Synonyms: CAY10618) 纯度: ≥99.0%

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。

GPP78(Synonyms: CAY10618)

GPP78 Chemical Structure

CAS No. : 1202580-59-3

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5 mg (11.38 mM * 1 mL in Methanol) ¥5400 In-stock

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生物活性

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]

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

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

参考文献
  • [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.

    [2]. Esposito E, et al. The NAMPT inhibitor FK866 reverts the damage in spinal cord injury. J Neuroinflammation. 2012 Apr 10;9:66.

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