SF2312

SF2312, a natural phosphonate antibiotic (Antibiotic), is a highly potent Enolase inhibitor with IC50s of 37.9 nM and 42.5 nM for human recombinant ENO1 and ENO2, respectively. SF2312 is active against bacteria under anaerobic conditions.

SF2312 is selectively toxic to ENO1-deleted glioma cells. SF2312 inhibits the proliferation (2 weeks treatment course) of the ENO1-deleted D423 glioma cell line in the low μM range whist isogenically ENO1-rescued D423 cells, ectopically re-expressing ENO1 only shows inhibition of proliferation at concentrations of SF2312 above 200 μM. SF2312 (10 μM) dose-dependently reduces the conversion of U-¹³C glucose to ¹³C lactate in a manner selective for ENO1-deleted over ENO1-rescued or otherwise ENO1-intact glioma cells^[1].
SF2312 is produced by the actinomycete Micromonospora and is active against a range of bacteria, with strong activity against Salmonella and Staphylococcus, weak activity against E. coli, and no activity against fungi^[1].

References:
[1]. Paul G Leonard, et al. SF2312 is a natural phosphonate inhibitor of enolase. Nat Chem Biol. 2016 Dec;12(12):1053-1058.