Nampt-IN-20 is a nicotinamide phosphoribosyltransferase ( Nampt ) inhibitor with a IC50 of 9.0 nM. Nampt-IN-20 binds to the active site of Nampt, occupies the NAM-binding region and disrupts NAD biosynthesis. Nampt-IN-20 exerts antiproliferative effects in A2780 ovarian cancer cells. Nampt-IN-20 can be used for the research of ovarian cancer [1].
In Vitro, Nampt-IN-20 (compound 7) potently inhibits purified Nampt protein with an IC50 of 9.0 nM[1]. Nampt-IN-20 potently inhibits A2780 ovarian cancer cell proliferation with an IC50 of 0.010 μM[1]. Nampt-IN-20 (30 minutes) shows low stability in mouse liver microsomes, with only 1.9% remaining after 30 minutes[1]. Nampt-IN-20 (30 minutes) shows moderate stability in human liver microsomes, with 44% remaining after 30 minutes[1].
References:
[1]. Zheng X, et al. Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors. Journal of medicinal chemistry. 2013 Aug 22;56(16):6413-33.
In Vitro, Nampt-IN-20 (compound 7) potently inhibits purified Nampt protein with an IC50 of 9.0 nM[1]. Nampt-IN-20 potently inhibits A2780 ovarian cancer cell proliferation with an IC50 of 0.010 μM[1]. Nampt-IN-20 (30 minutes) shows low stability in mouse liver microsomes, with only 1.9% remaining after 30 minutes[1]. Nampt-IN-20 (30 minutes) shows moderate stability in human liver microsomes, with 44% remaining after 30 minutes[1].
References:
[1]. Zheng X, et al. Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors. Journal of medicinal chemistry. 2013 Aug 22;56(16):6413-33.