| Bioactivity | Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor[1]. |
| Target | DNA gyrase, Topoisomerase IV |
| Invitro | Antibacterial agent 138 (compound 7a) 抑制来自不同微生物中的 DNA 促旋酶和拓扑异构酶 IV，表现出低纳摩尔范围的 IC50 值：金黄色葡萄球菌 (IC50 分别为 1.22 nM、8.0 nM)，大肠杆菌 (IC50 分别为 <10 nM、44 nM)，鲍曼不动杆菌 (IC50 分别为 2.42 nM、119.7 nM)，铜绿假单胞菌 (IC50 分别为 <10 nM、27.5 nM)[1]。Antibacterial agent 138 (≤100 μM) 对乳腺癌 MCF-7 细胞系和肝癌 HepG2 细胞无细胞毒性[1]。 |
| In Vivo | Antibacterial agent 138 (compound 7a) (25 and 50 mg/kg；静脉注射；单剂量) 对中性粒细胞减少的小鼠大腿感染模型有杀菌作用[1]。 |
| Name | DNA Gyrase-IN-6 |
| Formula | C18H16Cl2N4O4S |
| Molar Mass | 455.32 |
| 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]. Durcik M, et al. New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate Staphylococcus aureus. J Med Chem. 2023 Mar 23;66(6):3968-3994. |