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Chemical Structure : LPC-233
Catalog No.: PC-21019Not For Human Use, Lab Use Only.
LPC-233 (LPC233) is a highly potent and specific inhibitor of UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase LpxC (Ki=8.9 pM), specifically inhibits lipid A synthesis and displays outstanding antibiotic activities.
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LPC-233 (LPC233) is a highly potent and specific inhibitor of UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase LpxC (Ki=8.9 pM), specifically inhibits lipid A synthesis and displays outstanding antibiotic activities.
LPC-233 is a competitive inhibitor occupying the active site and substrate binding passage against the P. aeruginosa LpxC.
LPC-233 exhihits KI value of 0.22 ± 0.06 nM and 8.9 ± 0.5 pM for the encounter complex EI and stable complex EI*, respectively.
LPC-233 is broadly effective against a clinical collection of 285 strains of Gram-negative bacterial pathogens (MIC90<1.0 ug/mL), does not display detectable antibiotic activity toward Gram-positive bacteria, such as S. aureus, at 128 μg/mL.
LPC-233 has an MIC50 value of 0.064 μg/ml and an MIC90 value of 0.125 μg/ml against 151 extended spectrum β-lactamase (ESBL)–negative, carbapenemase-negative Enterobacteriaceae isolates.
LPC-233 displays identical MIC50 and MIC90 values against 42 ESBL, carbapenemase-producing isolates that are resistant to antibiotics.
LPC-233 does not substantially inhibit human MMPs (MMP-1, MMP-2, MMP-3, MMP-7, MMP-8. MMP-9, MMP-12, MMP-13, and MMP-14) and TACE at 30 uM.
LPC-233 demonstrates in vivo efficacy in multiple murine infection models, displays no cardiovascular toxicity in vivo.
| M.Wt | 376.36 | |
| Formula | C19H18F2N2O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jinshi Zhao, et al. Sci Transl Med. 2023 Aug 9;15(708):eadf5668.
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