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CHS-828 nicotinate is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 nicotinate (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity[1]. | [References]
[1] Watson M, et al. The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors. Mol Cell Biol. 2009 Nov;29(21):5872-88. DOI:10.1128/MCB.00112-09
[2] Cerna D, et al. 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. 2012 Jun 22;287(26):22408-17. DOI:10.1074/jbc.M112.357301 |
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