货号:A233155
同义名:
CI 919;AT 2266
Enoxacin is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent.
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产品名称 | Topo I ↓ ↑ | Topo II ↓ ↑ | Topo IV ↓ ↑ | Topoisomerase ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ellagic acid | ✔ | 99%+ | |||||||||||||||||
β-Lapachone | ✔ | 99%+ | |||||||||||||||||
(s)-10-hydroxycamptothecin | ✔ | 99%+ | |||||||||||||||||
Camptothecin |
++
Topo I, IC50: 0.68 μM |
98% | |||||||||||||||||
Betulinic acid |
++
Eukaryotic topoisomerase I, IC50: 5 μM |
99%+ | |||||||||||||||||
Topotecan |
++++
Topo I (DU-145 Luc cells), IC50: 2 nM Topo I (MCF-7 Luc cells), IC50: 13 nM |
99%+ | |||||||||||||||||
Irinotecan HCl Trihydrate | ✔ | 98% | |||||||||||||||||
SN-38 | ✔ | 98% | |||||||||||||||||
Levofloxacin hydrate | ✔ | 99%+ | |||||||||||||||||
Dexrazoxane | ✔ | 99%+ | |||||||||||||||||
Ofloxacin | ✔ | 98+% | |||||||||||||||||
Enoxacin | ✔ | 99%+ | |||||||||||||||||
Flumequine |
+
Topo II, IC50: 15 μM |
99%+ | |||||||||||||||||
Levofloxacin | ✔ | 99%+ | |||||||||||||||||
Etoposide | ✔ | 98% | |||||||||||||||||
Pefloxacin mesylate dihydrate | ✔ | 99+% | |||||||||||||||||
Marbofloxacin | ✔ | 99%+ | |||||||||||||||||
Voreloxin HCl | ✔ | 98% | |||||||||||||||||
Mitoxantrone dihydrochloride | ✔ | PKC | 99%+ | ||||||||||||||||
Nalidixic acid | ✔ | 99%+ | |||||||||||||||||
Doxorubicin | ✔ | 98% | |||||||||||||||||
Novobiocin sodium | ✔ | 98%+ | |||||||||||||||||
Amonafide | ✔ | 99%+ | |||||||||||||||||
Pirarubicin | ✔ | 98%+ | |||||||||||||||||
Idarubicin HCl |
+++
Topo II (MCF-7 cells), IC50: 3.3 ng/mL |
99%+ | |||||||||||||||||
Genistein | ✔ | EGFR | 98% | ||||||||||||||||
Teniposide | ✔ | 98% | |||||||||||||||||
Moxifloxacin | ✔ | 98% | |||||||||||||||||
Ciprofloxacin | ✔ | 99%+ | |||||||||||||||||
Clinafloxacin | ✔ | 97% | |||||||||||||||||
Gatifloxacin | ✔ | 99%+ | |||||||||||||||||
Daunorubicin HCl |
+++
DNA synthesis, Ki: 20 nM |
98% | |||||||||||||||||
Epirubicin HCl | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Enoxacin (AT 2266) is a fluoroquinolone antibiotic, which disrupts bacterial DNA by inhibiting DNA gyrase and topoisomerase IV, with IC50 values of 126 µg/ml and 26.5 µg/ml, respectively. It also functions as a miRNA processing activator, enhancing siRNA-mediated mRNA degradation and promoting the biogenesis of endogenous miRNAs. Enoxacin exhibits potent antibacterial activity against both gram-positive and gram-negative bacteria and acts as a cancer-specific growth inhibitor by boosting TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing[1].[2].[3].[4]. |
体内研究 | Furthermore, in an in vivo study, in GFP transgenic mice, Enoxacin administered at 100 µM in a volume of 2 µl directly into the ear once a day for three consecutive days (days 12, 13, and 14), significantly enhances GFP mRNA knockdown efficiency mediated by Lv-siGFP (from 80% to 60%; leaving 40% GFP mRNA levels), while having no effect on GFP expression when administered alone in the GFP transgenic line C57BL/6-Tg(ACTB-EGFP)1Osb/J (aged 10 days) with lentivirus expressing shGFP (Lv-siGFP; injected into the ear for 10 days)[3]. |
体外研究 | In cell-based assays, Enoxacin increases siGFP-mediated gene knockdown in a dose-dependent manner within a HEK293 cells-based reporter system, showing an effective concentration (EC50) of about 30 µM. It specifically enhances the processing of miRNAs and the loading of siRNA duplexes onto RISCs in these cells at a concentration of 50 µM[3]. Enoxacin does not affect the processing of pre-let-7 or pre-miR-30a by Dicer alone, but when combined with TRBP, it enhances their processing by Dicer[3]. Enoxacin is effective against various bacterial strains, inhibiting 90% of pathogens like Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at concentrations less than or equal to 0.8 micrograms/ml[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02099240 | Osteomyelitis | Early Phase 1 | Recruiting | September 2019 | United States, Kentucky ... 展开 >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD 502-852-1148 jarami01@louisville.edu Contact: David Seligson, MD 502-852-0923 d0seli01@louisville.edu Sub-Investigator: Forest Arnold, DO Sub-Investigator: Timothy Wiemkwn, PhD Sub-Investigator: Robert Kelley, PhD Sub-Investigator: James Summersgill, PhD Sub-Investigator: Ruth Carrico, PhD Sub-Investigator: Julie Harting, PharmD Sub-Investigator: Paula Peyrani, MD Principal Investigator: David Seligson, MD Sub-Investigator: Craig Roberts, MD Principal Investigator: Julio Ramirez, MD 收起 << |
NCT02305342 | - | Completed | - | Pakistan ... 展开 >> Research facility ID ORG-001126 Karachi, Pakistan, 75190 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.12mL 0.62mL 0.31mL |
15.61mL 3.12mL 1.56mL |
31.22mL 6.24mL 3.12mL |
CAS号 | 74011-58-8 |
分子式 | C15H17FN4O3 |
分子量 | 320.319 |
别名 | CI 919;AT 2266;Sesquihydrate, Enoxacin;Rhône-Poulenc Rorer Brand of Enoxacin Sesquihydrate;Brand of Enoxacin Sesquihydrate;Sesquihydrate Rhône Poulenc Rorer;Pierre Fabre Brand of Enoxacin;Enoxacino;Comprecin;Enoxacine;Penetrex;NSC 629661;Pd107779 |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 | |
动物实验配方 |