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CHIR-090

SKU: orb1303872

Description

CHIR-090 is a potent and selective small molecule inhibitor of the LpxC enzyme, exhibiting antibiotic activity. It is a valuable research tool for studying Gram-negative bacterial infections and peptidoglycan biosynthesis in both in vitro and in vivo experimental models.

Research Area

Infectious Disease & Virology

Images & Validation

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CHIR-090

Key Properties

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CAS Number728865-23-4
MW437.49
Purity96.10%
FormulaC24H27N3O5
SMILESC[C@@H](O)[C@H](NC(=O)c1ccc(cc1)C#Cc1ccc(CN2CCOCC2)cc1)C(=O)NO
TargetAntibacterial,Antibiotic
Solubility10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (2.29 mM);DMSO:60 mg/mL (137.15 mM)

Bioactivity

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Target IC50
LpxC:4.0 nM. (Ki)
In Vivo
CHIR-090 is a potent E. coli antibiotic, demonstrating significant E. coli LpxC inhibition within the low nanomolar (nM) range in vitro. Notably, E. coli W3110 colonies resistant to a 1 μg/mL concentration of CHIR-090 do not occur unless subjected to prior chemical mutagenesis. However, a specific strain of E. coli W3110 can grow on LB agar with CHIR-090 concentrations ranging from 1 to 10 μg/mL, which is significantly higher (4 to 40 times) than the minimum inhibitory concentration (MIC) of 0.25 μg/mL identified under our conditions for the wild-type E. coli W3110. The growth rate of W3110RL strain is unaffected by 1 μg/mL CHIR-090, maintaining a doubling time of 40 minutes, identical to that of the wild-type strain without the inhibitor. Conversely, the wild-type strain ceases growth approximately two hours after exposure to 1 μg/mL of CHIR-090.
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In Vitro
CHIR-090 is a highly effective, slow, tight-binding inhibitor targeting the LpxC deacetylase from Aquifex aeolicus, displaying significant antibiotic properties against Gram-negative pathogens like P. aeruginosa and E. coli. Its mode of action includes a two-step slow, tight-binding inhibition mechanism against E. coli LpxC, with an inhibition constant (Ki) of 4 nM, indicating potent activity at low nanomolar concentrations against LpxC orthologues from a range of Gram-negative bacteria including Pseudomonas aeruginosa, Neisseria meningitidis, and Helicobacter pylori. Contrarily, CHIR-090 exhibits weaker inhibition against LpxC from Rhizobium leguminosarum (Ki=340 nM), demonstrating a reduced efficacy and conventional inhibition pattern without the slow, tight-binding characteristic. This differential inhibition renders E. coli strains with LpxC from R. leguminosarum resistant to CHIR-090, even at concentrations 400 times the minimal inhibitory concentration effective against wild-type E. coli. Nevertheless, CHIR-090 showcases outstanding antibiotic efficacy against select pathogens, on par with ciprofloxacin, emphasizing its potential as a therapeutic agent.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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CHIR090, CHIR-090, CHIR 090, Bacterial, Inhibitor, inhibit

Similar Products

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  • CHIR-090

    CHIR-090 [orb1223063]

    >98% (HPLC)

    728865-23-4

    437.19

    C24H27N3O5

    1 g, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 500 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID
11546620 ↗

Key Properties

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No computed properties available.

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CHIR-090 (orb1303872)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 80.00
1 ml x 10 mM (in DMSO)
$ 140.00
5 mg
$ 140.00
10 mg
$ 200.00
25 mg
$ 380.00
50 mg
$ 580.00
100 mg
$ 820.00
500 mg
$ 1,620.00
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