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CHIR-090

Cat No.
CEI-1278
Description
CHIR-090 is a potent inhibitor of LpxC
Product Overview
CHIR-090 is a very potent, low, tight-binding inhibitor of LpxC with Ki value of 4.0 nM. LpxC is a zinc-dependent amidase and present in almost all Gram-negative bacteria. LpxC is a promising target for the development of novel antibiotic substances against multigrug-resistant Gram-negative bacteria. CHIR-090 is a potent LpxC inhibitor and has a different selectivity with the reported LpxC inhibitor L-161.When tested with Escherichia coli LpxC, administration of CHIR-090 showed tight inhibition with Ki value of 4.0 nM, Ki*=0.5 nM, K5=1.9/min and K6=0.18/min. In bacterial P. aeruginosa efflux pupm mutants, CHIR-090 treatment showed inhibition function on MexAB-Oprm, MexCD-OprJ and MexEF-OprN. CHIR-090 showed remarkable antibiotic activity against both E. coli and P. aeruginosa by inhibiting LpxC orthologs at low nM concentrations. In E. coli W3110RL with R. legumunosarum lpxC replacement of E. coli lpxC, CHIR-090 (1 to 10 μg/ml) treatment had no effect on strain growth on LB agar plates while wild-type cells stopped growing after about 2 h in the presence of 1 μg/ml CHIR-090.
CAS No.
728865-23-4
Molecular Weight
437.49
Purity
0.9868
Storage
Store at -20°C
Synonyms
CHIR 090; CHIR090
Targets
LpxC
Molecular Formula
C24H27N3O5
Chemical Name
N-[(2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl]-4-[2-[4-(morpholin-4-ylmethyl)phenyl]ethynyl]benzamide
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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