WebCHIR-090, a novel N -aroyl- l -threonine hydroxamic acid, is a potent, slow, tight-binding inhibitor of the LpxC deacetylase from the hyperthermophile Aquifex aeolicus, and it has excellent antibiotic activity against Pseudomonas aeruginosa and Escherichia coli, as judged by disk diffusion assays. Webchir-090 Synonym(s) : CHIR 090, CHIR090, N-((2S,3R)-3-Hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl)-4-((4-(morpholinomethyl)phenyl)ethynyl)benzamide, N-[(1S,2R)-2 …

CHIR-090 ≥98% (HPLC) Sigma-Aldrich

WebDec 20, 2024 · Upregulated expression of efflux pumps, lpxC target mutations, LpxC protein overexpression, and mutations in fabG were previously shown to mediate single-step resistance to the LpxC inhibitor CHIR-090 in P. aeruginosa Single-step selection experiments using three recently described LpxC inhibitors (compounds 2, 3, and 4) and … WebCHIR-090 is a slow, tight-binding inhibitor ofE. coli LpxC with Ki) 4.0 nM, Ki* ) 0.5 nM, k5) 1.9 min-1, and k6) 0.18 min-1. CHIR-090 inhibits LpxC orthologues from several other … tss notes

Mutations Reducing In Vitro Susceptibility to Novel LpxC ... - PubMed

WebCHIR-090 inhibits a wide range of LpxC enzymes with sub-nanomolar affinity in vitro, and is a two-step, slow, tight-binding inhibitor of Aquifex aeolicus and E. coli LpxC. The success of CHIR-090 suggests that potent LpxC-targeting antibiotics may be developed to control a broad range of Gram-negative bacteria. Publication types Review WebCHIR-090 is a potent, low, tight-binding inhibitor of LpxC (UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase) (Ki = 4.0 nM). Antibacterial agent Formula: C₂₄H₂₇N₃O5 WebFeb 25, 2016 · CHIR-090 features a substituted biphenyl acetylene tail group that competes with the acyl chain of the LpxC substrate to occupy the hydrophobic substrate passage of the enzyme 14. tssniper directshow error