Topoisomerase II-IN-26
Topoisomerase II-IN-26 is a dual bacterial type II topoisomerase (Top II) inhibitor, with IC50 values of 0.081 μM and 0.093 μM against Staphylococcus aureus DNA gyrase and topoisomerase IV, respectively, and IC50 values of 0.906 μM and 0.103 μM against Escherichia coli DNA gyrase and topoisomerase IV, respectively. Topoisomerase II-IN-26 also shows high selectivity for human topoisomerase IIα. Topoisomerase II-IN-26 inhibits biofilm formation, reduces the metabolic activity of mature biofilms, exhibits activity against Staphylococcus aureus, MRSA strains, Escherichia coli and Acinetobacter baumannii, and possesses a post-antibiotic effect. Topoisomerase II-IN-26 can be used for the research of bacterial infections such as Staphylococcus aureus and MRSA.
For research use only. We do not sell to patients.
- Formula: C22H21BrF3N3O3
- Molecular Weight:512.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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DNA Gyrase 81 nM (IC50) |
TOPO IV 93 nM (IC50) |
Topoisomerase II-IN-26 (Compound 20) (0.004-4 μg/mL; 20 h) potently inhibits growth of S. aureus and MRSA strains with MIC values of 0.004-0.008 μg/mL, and moderately inhibits E. coli (MIC = 4 μg/mL) and A. baumannii (MIC = 2 μg/mL)[1].
Topoisomerase II-IN-26 (50 μM) has low cytotoxicity against HepG2 (50.8% residual activity at 50 μM) and HUVEC (78.4% residual activity at 50 μM) cells[1].
Topoisomerase II-IN-26 (8 × MIC) induces a 1-hour post-antibiotic effect in MRSA at 8 × MIC, temporarily suppressing bacterial growth after transient exposure[1].
Topoisomerase II-IN-26 (½ × MIC; 14 days) shows slower resistance development in MRSA than Gepotidacin (HY-16742), with only an 8-fold MIC increase over 14 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:embryos[1]
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Dosage:0.004 μg/mL (1 × MIC); 0.008 μg/mL (2 × MIC); 0.016 μg/mL (4 × MIC)
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Administration:immersion in E3 medium
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Result:Did not significantly improve embryo survival relative to the untreated group at 1 × MIC.
Reduced bacterial load at 24 hours post-infection at 1 × MIC.
Significantly increased the survival rate of infected zebrafish embryos relative to the untreated group at 2 × MIC and 4 × MIC.
Chemical Information
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Molecular Weight 512.32
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Formula C22H21BrF3N3O3
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SMILES
COC1=NC2=C(N=CC(F)=C2OCC3CCC(CO3)NCC4=CC(F)=C(C(F)=C4)Br)C=C1
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Topoisomerase II-IN-26 Related Classifications
HY-184297 Related Classifications
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- Topoisomerase II-IN-26
- Topoisomerase
- Bacterial
- HepG2
- human topoisomerase IIα
- Staphylococcus aureus topoisomerase IV
- zebrafish embryos
- Escherichia coli DNA gyrase
- Staphylococcus aureus DNA gyrase
- MRSA strains
- Escherichia coli topoisomerase IV
- Acinetobacter baumannii
- bacterial type II topoisomerase
- Inhibitor
- inhibitor
- inhibit