Bederocin

Bederocin (up to 20 µM) does not inhibit the growth of A549 or H4IIE cells^[3].

Bederocin (15 minutes at 23°C) is a potent inhibitor of S. aureus MetS with an IC₅₀ <1.9 nM, while at 500 nM it shows no inhibitory effect on S. pneumoniae MetS2 or rat liver MRS^[2].
Bederocin increases the MIC from 0.12 μg/mL to 1 μg/mL in MetS-overexpressing S. aureus RN4220 (pYH4-metS), confirming target specificity^[2].
Bederocin (1-32 μg/mL; 48 hours) has an MPC of 32 μg/mL in S. aureus strains, including MRSA^[2].
Bederocin MIC increases from 0.015-0.06 μg/mL to 0.06-16 μg/mL in 19 Staphylococcus and Streptococcus strains^[2].
Bederocin inhibits the growth of S. aureus with an MIC of 0.12 µg/mL, whereas reagent-resistant mutant strains have an MIC of 2-32 µg/mL^[3].
Bederocin (20-24 h) shows potent broth microdilution activity against contemporary Gram-positive isolates, with an MIC₉₀ of 0.12 µg/mL for S. aureus, an MIC₉₀ of 0.12 µg/mL for S. epidermidis, an MIC₉₀ of 0.12 µg/mL for S. pyogenes, and MIC₉₀ values of 0.015 µg/mL or lower for enterococci^[4].

Bederocin (0.05 nM-1 µM; 30 min) inhibits wild-type S. aureus MetRS with an average K_i of 10 pM, showing competitive inhibition with respect to methionine and noncompetitive inhibition with respect to ATP^[3].
Bederocin (0.05 nM-1 µM) loses efficacy against S. aureus mutant MetRS enzymes, with G54A A64P showing up to a 190,000-fold increase in K_i compared with wild-type MetRS^[3].
Bederocin (K_i = 10 pM) inhibits purified S. aureus MetRS, exhibiting competitive inhibition with respect to methionine and noncompetitive inhibition with respect to ATP^[5].
Bederocin inhibits protein synthesis in S. pneumoniae, with RNA synthesis inhibition as a secondary stringent response effect^[5].