Type II topoisomerase inhibitor 1
Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area.
For research use only. We do not sell to patients.
- CAS No.: 2245691-60-3
- Formula: C18H15N3O4
- Molecular Weight:337.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
topoisomerase IV 0.98 μM (IC50) |
DNA gyrase 1.7 nM (IC50) |
In Vitro
Type II topoisomerase inhibitor 1 (13 e, 18 h) shows antibacterial activities against E. coli and S. aureus (MIC: 64 and 16 μg/mL, respectively)[1].
Type II topoisomerase inhibitor 1 (50 μM, 48 h) shows an 8.4% inhibition rate for HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:10, 50 μM
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Incubation Time:10, 50 μM
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Result:Showed cytoxicity with inhibition rates of 8.4% at 50 μM, 1.5% at 10 μM.
Chemical Information
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CAS No. 2245691-60-3
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Molecular Weight 337.33
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Formula C18H15N3O4
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SMILES
CNC1=CC=CC2=C1NC(C(C(NC3=CC=C(C=C3)C(O)=O)=O)=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Fumihito Ushiyama, et al. Lead Identification of 8-(Methylamino)-2-oxo-1,2-dihydroquinoline Derivatives as DNA Gyrase Inhibitors: Hit-to-Lead Generation Involving Thermodynamic Evaluation. ACS Omega. 2020 Apr 24;5(17):10145-10159. [Content Brief]
[2]. Fumihito Ushiyama, et al. Lead optimization of 8-(methylamino)-2-oxo-1,2-dihydroquinolines as bacterial type II topoisomerase inhibitors. Bioorg Med Chem. 2020 Nov 15;28(22):115776. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Type II topoisomerase inhibitor 1 Related Classifications
HY-150044 Related Classifications
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