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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
−20°C
SMILES 字串
Clc1ccc(cc1)OCCCCCCN\C(=N\C#N)\Nc2ccncc2
InChI
1S/C19H22ClN5O/c20-16-5-7-18(8-6-16)26-14-4-2-1-3-11-23-19(24-15-21)25-17-9-12-22-13-10-17/h5-10,12-13H,1-4,11,14H2,(H2,22,23,24,25)
InChI 密鑰
BOIPLTNGIAPDBY-UHFFFAOYSA-N
應用
GMX1778 has been used as NAMPT inhibitor, to study its effects on nicotinamide adenine dinucleotide (NAD) contents of SH-SY5Y cells exposed to Vacor.
生化／生理作用
GMX1778 (CHS-828) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) that exhibits a potent anticancer activity both in vitro and in vivo. GMX1778 exerts a cytotoxic effect by decreasing the cellular level of NAD+. GMX1778 increases intracellular ROS in cancer cells but does not induce ROS in normal cells.
GMX1778 can regulate redox status and has the ability to simulate ROS in cancer cells.
GMX1778 is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT).
訊號詞
Warning
危險分類
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
標靶器官
Respiratory system
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Identification of the nicotinamide salvage pathway as a new toxification route for antimetabolites
Buonvicino D, et al.
Cell Chemical Biology, 25(4), 471-482 (2018)
Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53-and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner
Cerna D, et al.
The Journal of Biological Chemistry, 287(26), 22408-22417 (2012)
Daniela Buonvicino et al.
Cell chemical biology, 25(4), 471-482 (2018-02-27)
Interest in the modulation of nicotinamide adenine dinucleotide (NAD) metabolome is gaining great momentum because of its therapeutic potential in different human disorders. Suppression of nicotinamide salvage by nicotinamide phosphoribosyl transferase (NAMPT) inhibitors, however, gave inconclusive results in neoplastic patients because
Chiara Zucal et al.
BMC cancer, 15, 855-855 (2015-11-07)
Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme in NAD(+) biosynthesis from nicotinamide, is one of the major factors regulating cancer cells metabolism and is considered a promising target for treating cancer. The prototypical NAMPT inhibitor FK866 effectively lowers NAD(+) levels in
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