SF2312 (SF 2312) is a highly potent inhibitor of Enolase with IC50 of 37.9 and 42.5 nM for recombinant hENO1 and hENO2, respectively.
SF2312 previously isolated as natural phosphonate antibiotic of unknown mode of action.
SF2312 exhibits non-competitive kinetics with respect to substrate 2-PGA but competitive kinetics at higher concentrations of inhibitor.
SF2312 is selectively toxic to ENO1-deleted glioma cells in the low μM range.
SF2312 (10 uM) selectively blocks glycolysis in ENO1-deleted glioma cells.
SF2312 proved superior to PhAH for killing ENO1-deleted versus ENO1-rescued glioma cells, especially under anaerobic conditions.
