STF-31
NAMPT inhibitor / STF31 is an inhibitor of glucose transporter 1 (GLUT1; IC50 = 1 µM)1 and NAMPT3. Inhibition of glucose transporters to target It has been shown to kill renal cell carcinoma cells (the majority of which lack the von Hippel-Lindau suppressor gene) without toxicity to normal cells. The target of STF31 anti-tumor activity has recently been questioned via use of large-scale cancer cell-line profiling.2 This profiling indicated that nicotinamide phosphoribosyltransferase (NAMPT) was in fact the target of STF31. The inhibition of NAMPT by STF31 was confirmed via biochemical assay against recombinant NAMPT. The ability of STF31 to inhibit NAMPT had been previously displayed (IC50 = 19 nM).3
Biochemicals & reagents
724741-75-7
1) Chan et al. (2011), Targeting GLUT1 and the Warburg effect in renal cell carcinoma by chemical synthetic lethality; Sci.Transl.Med. 3 94ra70 2) Adams et al., (2014), NAMPT is the Cellular Target of STF-31-Like Small-Molecule Probes; ACS Chem.Biol. 9 2447 3) Dragovich et al. (2014), Fragment-based design of 3-aminopyridine-derived amides as potent inhibitors of human nicotinamide phosphribosyltransferase (NAMPT); Bioorg.Med.Chem.Lett. 24 954
-20°C
TARGET: Energy production -- PATHWAY: Carbohydrate metabolism; NAD, NADP pathways -- DISEASE AREA: Cancer