MRL-494 hydrochloride 是一种抗菌剂，是一种 BamA 的抑制剂，具有抗外排和外膜渗透性。MRL-494 hydrochloride 可抑制革兰氏阳性细菌 (金黄色葡萄球菌 COL 的 MIC 值为 12.5 μM) 和革兰氏阴性细菌 (大肠杆菌 JCM158 的 MIC 值为 25 μM)。
MRL-494 hydrochloride, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 hydrochloride can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias[1].
MRL-494 lethally disrupts the cytoplasmic membrane. MRL-494 inhibits OM proteins (OMPs) biogenesis from outside the outer membrane (OM) by targeting BamA. MRL-494 exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of MRL-494 against E. coli (WT), E. coli (δtolC), E. coli (δtolC envA101), K. pneumonia, A. baumannii (WT), A. baumannii (δlpxC) , P. aeruginosa (efflux deficient), P. aeruginosa (WT), Staphylococcus aureus (methicillin-resistant) and Bacillus subtilis rpoB18 are 25 μM, 25 μM, 25 μM, 100 μM, 200 μM, 200 μM, 100 μM, 100 μM, 12.5 μM and 25 μM, respectively[1].
[1]. Hart EM, A small-molecule inhibitor of BamA impervious to efflux and the outer membrane permeability barrier. Proc Natl Acad Sci U S A. 2019 Oct 22;116(43):21748-21757.
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