TABLE 1

Susceptibility of bacterial strains to MsbA inhibitors

ParameteraStrainbValue for the parameter with:c
G592G913G332
Biochemical IC50 (nM)Purified E. coli MsbA150 ± 483.8 ± 0.982.8 ± 0.75
EC50 (μM)CFT073 lptD(imp4213) msbAlow4.5 ± 2.90.15 ± 0.0450.11 ± 0.032
CFT073 lptD(imp4213) msbAWT8.3 ± 2.70.27 ± 0.0750.19 ± 0.04
CFT073 lptD(imp4213) msbAhigh40 ± 231.1 ± 0.400.46 ± 0.16
MIC (μg/ml)CFT073 lptD(imp4213)21 ± 160.24 ± 0.130.22 ± 0.11
CFT073 ΔtolC18 ± 50.22 ± 0.150.31 ± 0.22
CFT073 WT>4139 ± 112.8 ± 0
K. pneumoniae ATCC 700721ND>452.8 ± 0
E. cloacae ATCC 13047ND>452.8 ± 0
  • a IC50, 50% inhibitory concentration.

  • b Low and high levels of MsbA expression are indicated by msbAlow and msbAhigh, respectively; wild-type expression is indicated as msbAWT.

  • c For all samples, n ≥ 3. ND, not determined.