CHIR-090 NEW
| Price | $40 | $97 | $157 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: CHIR-090 | CAS No.: 728865-23-4 |
| Purity: 97.29% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | CHIR-090 |
| Description | CHIR-090 is a very potent and selective LpxC inhibitor with antibiotic activity. |
| Kinase Assay | Disk diffusion is conducted, except that 10 μg of each antibiotic compound is used per filter. Growth in liquid medium in the presence of CHIR-090 is evaluated as follows: cells from overnight cultures are inoculated into 50 mL portions of LB broth at an A600 of 0.02 and grown with shaking at 30°C. When the A600 reaches 0.15, parallel cultures are treated with either 6 μL of 500 μg/mL CHIR-090 in DMSO or 6 μL of DMSO. To assess cumulative growth, cultures are maintained in log phase growth by 10-fold dilution into pre-warmed medium, containing the same concentrations of DMSO or DMSO/CHIR-090, whenever the A600 reaches 0.4. The minimal inhibitory concentration is defined as the lowest antibiotic concentration at which no measurable bacterial growth is observed in LB medium containing 1% DMSO (v/v), when inoculated at a starting density of A600=0.01. Cultures are incubated with shaking for 24 h at 30°C in the presence of CHIR-090. Experiments are performed in triplicate[1]. |
| 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. |
| 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[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 60 mg/mL (137.24 mM) |
| Keywords | Inhibitor | CHIR-090 | CHIR 090 | inhibit | Bacterial |
| Inhibitors Related | Neomycin sulfate | Dehydroacetic acid sodium | Ampicillin sodium | Methyl anthranilate | Doxycycline (hyclate) | Kanamycin sulfate | G-418 disulfate | Sulfamethoxazole sodium | Metronidazole | Doxycycline | Dimethyl sulfoxide | Crystal Violet |
| Related Compound Libraries | Bioactive Compound Library | Drug-induced Liver Injury (DILI) Compound Library | Antibiotics Library | Inhibitor Library | NO PAINS Compound Library | Anti-Bacterial Compound Library | Bioactive Compounds Library Max | Anti-Infection Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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