Kasugamycin sulfate
Based on 1 publication(s) in Google Scholar
Kasugamycin (Ksg) sulfate is an aminoglycoside antibiotic (antibiotic) that binds to the bacterial 30S ribosomal subunit and inhibits canonical translation initiation. Kasugamycin sulfate binds to the P-site and E-site codon regions in the mRNA channel and interferes with mRNA-tRNA codon-anticodon interactions, thereby destabilizing initiator tRNA binding. Kasugamycin sulfate possesses anti-infective activity. Kasugamycin sulfate is used in research on bacterial translation and Pseudomonas infection.
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- CAS No.: 78822-08-9
- Formule: C14H25N3O9.1/2H2O4S
- Masse moléculaire:428.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Kasugamycin sulfate
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Activité biologique
Description
In Vitro
Kasugamycin (Ksg) (100 mM) sulfate binds to the Thermus thermophilus 30S ribosomal subunit, forming two binding sites in the mRNA pathway; the primary binding site is located at the top of h44, between h24 and h28, and spans the P/E site region, while the secondary binding site is located adjacent to the E site and interacts with h23, h24 of 16S rRNA and ribosomal protein S7, with the Kasugamycin sulfate-30S complex structure determined at a resolution of 3.35 Å[2].
Kasugamycin (0-1 mM; 15 min; 37 °C) sulfate inhibits the binding of MVF-mRNA to Escherichia coli 30S ribosomal subunits and 70S ribosomes, with inhibition rates of 40% and 25% at 1 mM, respectively[2].
Kasugamycin (0-1 mM; 15 min; 37 °C) sulfate inhibits the binding of initiator fMet-tRNA to MVF-mRNA-programmed Escherichia coli 30S ribosomal subunits, with a maximum inhibition rate of 75% at 1 mM, while it has no significant effect on the binding of fMet-tRNA to 70S ribosomes[2].
Kasugamycin (500 μM; 15 min; 37 °C) sulfate inhibits the binding of leaderless mRNA and initiator fMet-tRNA to Escherichia coli 70S ribosomes by 29% and 13%, respectively, indicating that the 70S initiation complex formed by leaderless mRNA-fMet-tRNA is relatively insensitive to Kasugamycin sulfate[2].
Kasugamycin (12.5-50 μg/mL) sulfate inhibits 32 strains of Pseudomonas aeruginosa cultured in peptone water at pH 7.0, with 1 strain inhibited at 12.5 μg/mL, 19 strains inhibited at 25 μg/mL, and 12 strains inhibited at 50 μg/mL[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Kasugamycin (100 mg/kg; i.p.; single administration) sulfate achieves a 50% survival rate in mice infected intraperitoneally with mucin-containing Pseudomonas aeruginosa No. 87 (100 MLD)[4].
Kasugamycin (200 mg/kg; i.p.; single administration) sulfate achieves a 75% survival rate in mice infected intraperitoneally with mucin-containing Pseudomonas aeruginosa No. 87 (100 MLD)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice were intraperitoneally inoculated with Pseudomonas aeruginosa No. 87 with mucin at 1 MLD.[4]
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Dosage:200 mg/kg
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Administration:i.p.; single injection
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Result:Resulted in 100% survival.
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Animal Model:Mice were intraperitoneally inoculated with Pseudomonas aeruginosa No. 87 with mucin at 1 MLD.[4]
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Dosage:100 mg/kg
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Administration:i.p.; single administration
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Result:Resulted in 50% survival.
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Animal Model:Mice were intraperitoneally inoculated with Pseudomonas aeruginosa No. 87 with mucin at 1 MLD.[4]
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Dosage:200 mg/kg
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Administration:i.p.; single administration
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Result:Resulted in 75% survival.
Chemical Information
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CAS No. 78822-08-9
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Masse moléculaire 428.40
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Formule C14H25N3O9.1/2H2O4S
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SMILES
OS(=O)(O)=O.OC(C(N[C@@H](C[C@@H]1N)[C@@H](C)O[C@]1([H])O[C@@H]2[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@H]2O)=N)=O.[1/2]
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Synonyms
Ksg sulfate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Front Mol Biosci
Discovery of Kasugamycin as a Potent Inhibitor of Glycoside Hydrolase Family 18 Chitinases. [Abstract]2021 Apr 7:8:640356. PMID: 33898519
Pureté et documentation
Références
[1]. Zhang H, et al. Simultaneous determination of kasugamycin and validamycin-A residues in cereals by consecutive solid-phase extraction combined with liquid chromatography-tandem mass spectrometry. Food additives & contaminants. Part A, Chemistry, analysis, control, exposure & risk assessment. 2018 Mar;35(3):487-497. [Content Brief]
[2]. Schluenzen F, et al. The antibiotic kasugamycin mimics mRNA nucleotides to destabilize tRNA binding and inhibit canonical translation initiation. Nature structural & molecular biology. 2006 Oct;13(10):871-8. [Content Brief]
[3]. Kasuga K, et al. Heterologous production of kasugamycin, an aminoglycoside antibiotic from Streptomyces kasugaensis, in Streptomyces lividans and Rhodococcus erythropolis L-88 by constitutive expression of the biosynthetic gene cluster. Applied microbiology and biotechnology. 2017 May;101(10):4259-4268. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)