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Nampt (mouse) (rec.) (enzymatically active) (AG-40B-0179) is inhibited by the specific Nampt inhibitor CHS-828 (AG-CR1-0064). Methods: The protein Nampt (mouse) (rec.) (1µM) is tested for activity in vitro using the Cyclex NAMPT Colorimetric Assay Kit (Cyclex / MBL, CY-1251) in the presence of different concentrations of CHS-828 (dissolved in DMSO). The IC50 of CHS-828 is 40nM in this experiment.
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Temporal effects of the novel antitumour pyridyl cyanoguanidine (CHS 828) on human lymphoma cells: P. Martinsson, et al.; Eur. J. Cancer 37, 260 (2001)
Cyanoguanidine CHS 828 induces programmed cell death with apoptotic features in human breast cancer cells in vitro: C.M. Hansen, et al.; Anticancer Res. 20, 4211 (2000)
Cell death with atypical features induced by the novel antitumoral drug CHS 828, in human U-937 GTB cells: P. Martinsson, et al.; Eur. J. Pharmacol. 417, 181 (2001)
Model for time dependency of cytotoxic effect of CHS 828 in vitro suggests two different mechanisms of action: S.B. Hassan, et al.; J. Pharmacol. Exp. Ther. 299, 1140 (2001)
Action of a novel anticancer agent, CHS 828, on mouse fibroblasts: increased sensitivity of cells lacking poly (ADP-Ribose) polymerase-1: H. Lövborg, et al.; Cancer Res. 62, 4206 (2002)
A Phase I study of CHS 828 in patients with solid tumor malignancy: P. Hovstadius, et al.; Clin. Cancer Res. 8, 2843 (2002)
Activation of p53 protein in normal and in tumor cells by a novel anticancer agent CHS 828: J. Wojciechowski, et al.; Drugs Exp. Clin. Res. 29, 53 (2003)
Anticancer agent CHS 828 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity: L.S. Olsen, et al.; Int. J. Cancer 111, 198 (2004)
Novel antiproliferative antitumor agents: M.M. Mader, et al.; Curr. Opin. Drug Discov. Devel. 8, 613 (2005)
CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome: S.B. Hassan, et al.; Anticancer Res. 26, 4431 (2006)
Anticancer agent CHS-828 inhibits cellular synthesis of NAD: U.H. Olesen, et al.; BBRC 367, 799 (2008)
Structure-activity relationship analysis of cytotoxic cyanoguanidines: selection of CHS 828 as candidate drug: H. Lövborg, et al.; BMC Res. Notes 2, 114 (2009)
The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors: M. Watson, et al.; Mol. Cell. Biol. 29, 5872 (2009)
Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase: U.H. Olesen, et al.; BMC Cancer 10, 677 (2010)
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