Bioactivity | 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]. |
Invitro | 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: |
Name | Type II topoisomerase inhibitor 1 |
CAS | 2245691-60-3 |
Formula | C18H15N3O4 |
Molar Mass | 337.33 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |