產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 10mg 50mg
CAS	200484-11-3
別名
化學(xué)名	(Z)-2-(6-(4-chlorophenoxy)hexyl)-1-cyano-3-(pyridin-4(1H)-ylidene)guanidine
分子式	C19H22ClN5O
分子量	371.86
溶解度	≥ 18.3mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

GMX1778 (CHS828) is a potent and specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with a Kd value of 120 nM [1].

NAMPT is an NAD+ biosynthesis enzyme. NAD+ is a cofactor of enzymatic redox reactions that are involved in cellular metabolism, including ATP production. NAD+ is also important in many cellular pathways responsible for gene regulation, calcium homeostasis, genomic integrity, longevity and apoptosis. Cancer cells are significantly dependent on NAD+ for supporting high levels of ATP production for rapid cell proliferation [1].

Treatment with 30 nM GMX1778 for 6 h, extracts of IM-9 cells showed decreased NAD+ and NM levels, compared to cytosolic extracts of untreated cells. These levels continued to decrease throughout the rest of the time course experiment. The most profoundly changed was the metabolite NAD+ level. Between the 6- and 20-h time points, the decline of NAD+ occurred [1].

The NAD+ salvage pathway produces NAD+ using either nicotinic acid (niacin) (NA) or nicotinamide (niacinamide) (NM) as a substrate. NAPRT1 is short for NA phosphoribosyltransferase 1. On xenograft tumors derived from NAPRT1-proficient (HCT-116) and NAPRT1-deficient (HT1080) cell lines in mice, a 24-h iv infusion of GMX1777 at 150 mg/kg or 650 mg/kg produced antitumor activity. A 4-h iv infusion of NA at 120 mg/kg did not adversely affect the antitumor activity of GMX1777 in the NAPRT1-deficient xenograft, but abolished the antitumor activity of GMX1777 against the NAPRT1-proficient HCT-116 cell line [1].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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