LSN3154567;Nampt-IN-1;Nampt inhibitor 1;LSN3154567 (Nampt-IN-1);Nampt-IN-1, 10 mM in DMSO;LSN 3154567;LSN-3154567;LSN3154567;2-hydroxy-2-methyl-N-[1,2,3,4-tetrahydro-2-[2-(3-pyridinyloxy)acetyl]-6-;2-Hydroxy-2-methyl-N-[1,2,3,4-tetrahydro-2-[2-(3-pyridinyloxy)acetyl]-6-isoquinolinyl]-1-propanesulfonamide;2-hydroxy-2-methyl-N-(2-(2-(pyridin-3-yloxy)acetyl)-1,2,3,4-tetrahydroisoquinolin-6-yl)propane-1-sulfonamide;1-Propanesulfonamide, 2-hydroxy-2-methyl-N-[1,2,3,4-tetrahydro-2-[2-(3-pyridinyloxy)acetyl]-6-isoquinolinyl]-
Nampt-IN-1 is a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt; IC50 = 3.1 nM). It is selective for Nampt over a panel of greater than 100 human kinases at 1 μM. Nampt-IN-1 inhibits NAD+ formation in and proliferation of HCT116 cells (IC50s = 1.8 and 8.9 nM, respectively). It inhibits cell growth in a panel of cancer cell lines (IC50s = <0.2-2 μM). Nampt-IN-1 inhibits NAD+ formation in an A2780 ovarian carcinoma mouse xenograft model (ED50 = 2 mg/kg).
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Nampt-IN-1 functions as a co-drug. Nampt-IN-1 is a potent and selective NAMPT inhibitor.
Biochem/physiol Actions
LSN3154567 might be useful in developing a novel cancer therapeutic.
