| Description | G-418 disulfate (Geneticin sulfate) is an aminoglycoside antibiotic, an inhibitor of protein synthesis with eukaryotic selectivity. G-418 disulfate blocks peptide synthesis by inhibiting peptide chain elongation. |
| In vitro | 方法：仓鼠肾成纤维细胞 BHK-21、人宫颈癌细胞 HeLa、小鼠胚胎细胞 3T3 和仓鼠卵巢细胞 CHO-K1 用 G-418 disulfate (0-10000 µg/mL) 处理 24 h，使用 MTT 方法检测细胞生长抑制情况。结果：G-418 disulfate 剂量依赖性地抑制 BHK-21、HeLa、3T3 和 CHO-K1 细胞生长，IC50 分别为 69/483/213/311 µg/mL。[1]方法：人类永生成骨细胞 hFOB 1.19 在含有 G-418 disulfate (0.3 mg/mL) 的 DMEM/F12 培养基中培养。 结果：G-418 disulfate 维持 hFOB 1.19 细胞对 NEO 的抗性。[2]方法：质粒转染的人肺腺癌细胞 A549 用 G-418 disulfate (800 μg/ml) 筛选，偶尔用维持剂量的 G-418 disulfate (400 μg/mL) 处理。 结果：G-418 disulfate 筛选并维持带有 NEO 抗性的细胞。[3] |
| In vivo | 方法：为研究近端脊髓性肌萎缩 (SMA)的治疗，将 G-418 disulfate (14 mg/kg in saline) 腹腔注射给 dSMA 小鼠，每天一次，持续十二天。结果：G-418 disulfate 对 SMA 小鼠的处理增加了 SMN 蛋白和小鼠运动功能。[4]方法：为测定布鲁氏锥虫在体内对 G-418 的易感性水平，将 G-418 disulfate (10-80 mg/kg) 腹腔注射给 Trypanosoma brucei brucei 感染的小鼠，每天一次，持续三天。结果： G-418 disulfate (40-80 mg/kg) 可以在小鼠宿主中选择 G-418 抗性转染的Trypanosoma brucei brucei。[5] |
| Synonyms | Geneticin, G418 Sulfate, Antibiotic G-418 sulfate, 遗传霉素, Geneticin sulfate |
| molecular weight | 692.71 |
| Molecular formula | C20H40N4O10·2H2O4S |
| CAS | 108321-42-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 43.31 mM DMSO: Insoluble |
| References | 1. Delrue I, et al. Determination of the Selection Capacity of Antibiotics for Gene Selection. Biotechnol J. 2018 Aug;13(8):e1700747. 2. Ye G, et al. The FAP α -activated prodrug Z-GP-DAVLBH inhibits the growth and pulmonary metastasis of osteosarcoma cells by suppressing the AXL pathway. Acta Pharm Sin B. 2022 Mar;12(3):1288-1304. 3. Nasonovs A, et al. A549 cells contain enlarged mitochondria with independently functional clustered mtDNA nucleoids. PLoS One. 2021 Mar 25;16(3):e0249047. 4. Heier CR, et al. Translational readthrough by the aminoglycoside geneticin (G418) modulates SMN stability in vitro and improves motor function in SMA mice in vivo. Hum Mol Genet. 2009 Apr 1;18(7):1310-22. 5. Murphy NB, et al. Use of an in vivo system to determine the G418 resistance phenotype of bloodstream-form Trypanosoma brucei brucei transfectants. Antimicrob Agents Chemother. 1993 May;37(5):1167-70. |
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