BPH-1358 (NSC50460) free base is a potent human undecaprenyl diphosphatesynthase (UPPS) and farnesyldiphosphatesynthase (FPPS) inhibitor (IC50s: 110 nM and 1.8 μM) and is active against S. aureus in vitro (MIC ~250 ng mL).
The compound binds and blocks farnesyldiphosphatesynthase in the HMG-CoA pathway (IC50 = 460 nM for recombinant human FPPS). It causes macrophage apoptosis and inhibits prenylation and sterol biosynthesis in purified osteoclasts.