Type II topoisomerase inhibitor 1

Modify Date: 2025-10-15 18:00:02

Type II topoisomerase inhibitor 1 Structure
Type II topoisomerase inhibitor 1 structure
Common Name Type II topoisomerase inhibitor 1
CAS Number 2245691-60-3 Molecular Weight 337.33
Density N/A Boiling Point N/A
Molecular Formula C18H15N3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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[1][2].

 Names

Name Type II topoisomerase inhibitor 1

 Type II topoisomerase inhibitor 1 Biological Activity

Description 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[1][2].
Related Catalog
Target

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]. . Cell Viability Assay[1] Cell Line: HepG2 cells Concentration: 10, 50 μM Incubation Time: 10, 50 μM Result: Showed cytoxicity with inhibition rates of 8.4% at 50 μM, 1.5% at 10 μM.
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.

[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.

 Chemical & Physical Properties

Molecular Formula C18H15N3O4
Molecular Weight 337.33
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