CHS-828 (GMX-1778)
NAMPT inhibitor / A potent and selective inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme in the biosynthesis of NAD, which may be used to deplete cells of NAD.1 Displays potent cytotoxic effects in tumor cells.2,3 Displays antitumor activity in vivo.3 Increases ROS levels in cancer cells but not in normal cells.4
Biochemicals & reagents
200484-11-3
GMX-1778
1) Olesen et al. (2008), Anticancer agent CHS-828 inhibits cellular synthesis of NAD; Biochem.Biophys.Res.Commun. 376 799 2) Hassan et al. (2006), CHS 828 kill tumor cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome; Anticancer Res. 26 4431 3) Hjarnaa et al. (1999), CHS 828, a novel pyridyl cyanoguanidine with potent antitumor activity in vitro and in vivo; Cancer Res. 59 5751 4) Cerna et al. (2012) 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; J.Biol.Chem. 287 22408
-20°C
TARGET: Energy production -- PATHWAY: NAD, NADP pathways; Cytotoxicity; Cytokine; Chromatin -- RESEARCH AREA: Epigenetics; Stem cells; Cell death -- DISEASE AREA: Cancer