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^[1]. In Vitro: 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].