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Enoxacin hydrate

MCE China：Enoxacin hydrate

Brand：MedChemExpress (MCE)

Cat. No.HY-B0268A

CAS：84294-96-2

Synonyms：Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate

Purity：99.85%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 μg/ml) and topoisomerase IV (IC50=26.5 μg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.

In Vitro：Enoxacin hydrate (Enoxacin sesquihydrate) increases siGFP-mediated gene knockdown mediated by siRNA against EGFP in HEK293 cells-based reporter system in a dose-dependent manner, with a median effective concentration (EC50) of ~30 μM, whereas it has no effect on the cells expressing GFP only. Enoxacin (50 μM) promotes the processing of miRNAs and the loading of siRNA duplexes onto RISCs in HEK293 cells[3]. Enoxacin has no effect on the processing of pre-let-7 or pre-miR-30a by Dicer alone. However, the addition of Enoxacin can enhance the processing of let-7 or pre-miR-30a by Dicer and TRBP together[3]. Enoxacin inhibits 90% Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at less than or equal to 0.8 micrograms/ml[5].

In Vivo：Enoxacin hydrate (Enoxacin sesquihydrate; 100 μM; 2 μl; injected into ear once a day for 3 consecutive days (days 12, 13 and 14)) enhances the the GFP mRNA knockdown efficiency by Lv-siGFP (from 80% to 60%; 40% GFP mRNA level remained), whereas alone has no effect on GFP expression in GFP transgenic line C57BL/6-Tg(ACTB-EGFP)1Osb/J (10 d old) with lentivirus expressing shGFP (Lv-siGFP; injected into ear for 10 days)[3].

IC50 & Target：Quinolone

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References：

[1]. Sonia Melo, et al.Small molecule enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2-mediated microRNA processing. Proc Natl Acad Sci U S A. 2011 Mar 15;108(11):4394-9.  [Content Brief]

[2]. M Takei, et al. Target preference of 15 quinolones against Staphylococcus aureus, based on antibacterial activities and target inhibition. Antimicrob Agents Chemother. 2001 Dec;45(12):3544-7.  [Content Brief]

[3]. Ge Shan, et al. A small molecule enhances RNA interference and promotes microRNA processing. Nat Biotechnol. 2008 Aug;26(8):933-40.  [Content Brief]

[4]. Rengen Fan, et al. Small molecules with big roles in microRNA chemical biology and microRNA-targeted therapeutics. RNA Biol. 2019 Jun;16(6):707-718.  [Content Brief]

[5]. Chin, N.-X. and H.C. Neu, In vitro activity of enoxacin, a quinolone carboxylic acid, compared with those of norfloxacin, new beta-lactams, aminoglycosides, and trimethoprim. Antimicrobial agents and chemotherapy, 1983. 24(5): p. 754-763.  [Content Brief]