TABLE 1.

Inhibition of MetS activity by REP8839

MRS enzyme activityIC50 (nM)a
S. aureus MetS<1.9
H. influenzae MetG25
E. coli MetG307
S. pneumoniae MetS2>500
Rat liver lysateb>500
  • a The specific activity of individual enzyme preparations varied. Enzyme concentrations were adjusted to achieve charging of 15 to 25 pmol of tRNAMet in 15 min at 23°C. The enzyme concentrations were 1.5 nM for S. aureus, 3.0 nM for H. influenzae, 2.0 nM for E. coli, and 12 nM for S. pneumoniae MRS.

  • b Rat MRS concentration was not determined; the rat liver lysate catalyzed the charging of 5 pmol of tRNAMet in 15 min at 23°C.