Medchemexpress

Network Version

CHIR-090 Data Sheet

Product Name: CHIR-090
CAS No.: 728865-23-4
Cat. No.: HY-15460
MWt: 437.49
Formula: C24H27N3O5
Purity : >98%
Solubility: DMSO : 5 mg/mL (11.43 mM; Need ultrasonic)
Mechanisms: Target: Infection
Biological Activity:
CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase. It binds to E. coli LpxC with a Ki of 4.0 nM. CHIR-090 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target: Ki: 4 nM (Escherichia coli LpxC)[1] In Vitro: CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase from the hyperthermophile Aquifex aeolicus, and it has excellent antibiotic activity against P. aeruginosa and E. coli, as judged by disk diffusion assays. CHIR-090 is also a two-step slow, tight-binding inhibitor of Escherichia coli LpxC with Ki=4 nM. CHIR-090 at low nM levels inhibits LpxC orthologues from diverse Gram-negative pathogens, including Pseudomonas aeruginosa, Neisseria meningitidis, and Helicobacter pylori. In contrast, CHIR-090 is a relatively weak competitive and conventional inhibitor (lacking slow, tight-binding kinetics) of LpxC from Rhizobium leguminosarum (Ki=340 nM), a Gram-negative plant endosymbiont that is resistant to this compound. An E. coli construct in which the chromosomal lpxC gene is replaced by R. leguminosarum lpxC is resistant to CHIR-090 up to 100 μg/mL, or 400 times above the minimal inhibitory concentration for wild-type E. coli. CHIR-090, a very potent, slow, tight-binding inhibitor of Aquifex aeolicus LpxC, the sequence of which is 31 % identical to E. coli LpxC. CHIR-090 has remarkable antibiotic activity against E. coli and P. aeruginosa, comparable to ciprofloxacin, as judged by disk diffusion assays[1]. In Vivo: CHIR-090 is a potent antibiotic against E. coli and inhibits E. coli LpxC activity in vitro in the low nM range. E. coli W3110 colonies resistant to 1 μg/mL CHIR-090 are not observed without prior chemical mutagenesis. A strain of E. coli W3110 is able to grow on LB agar plates containing 1 to 10 μg/mL CHIR-090, which is 4 to 40 times above the MIC of 0.25 μg/mL under our conditions for wild-type E. coli W3110. The doubling time of W3110RL is 40 min in the presence of 1 μg/mL CHIR-090, which is exactly the same rate as wild-type in the absence of inhibitor. Wild-type cells stopped growing after about 2 h in the presence of 1 μg/mL CHIR-090[1].

Caution: Not fully tested. For research purposes only

Medchemexpress LLC

www.medchemexpress.com

1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA

Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Web:www.medchemexpress.com

Keywords: buy CHIR-090 | CHIR-090 Supplier | purchase CHIR-090 | CHIR-090 cost | CHIR-090 manufacturer | order CHIR-090 | CHIR-090 distributor | CHIR-090 structure buy 728865-23-4 | 728865-23-4 Supplier | purchase 728865-23-4 | 728865-23-4 cost | 728865-23-4 manufacturer | order 728865-23-4 | 728865-23-4 distributor | 728865-23-4 structure