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Elesclomol (STA-4783) 是一种氧化应激诱导剂,也是一种高度亲脂性的铜离子载体。Elesclomol 可以诱导肿瘤细胞凋亡,用于铜死亡相关研究。Elesclomol 还可以抑制 FDX1 介导的 Fe-S 簇生物合成。
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Elesclomol (STA-4783) 是一种氧化应激诱导剂,也是一种高度亲脂性的铜离子载体。Elesclomol 可以诱导肿瘤细胞凋亡,用于铜死亡相关研究。Elesclomol 还可以抑制 FDX1 介导的 Fe-S 簇生物合成。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 215 | 现货 | |
2 mg | ¥ 297 | 现货 | |
5 mg | ¥ 478 | 现货 | |
10 mg | ¥ 769 | 现货 | |
25 mg | ¥ 950 | 现货 | |
50 mg | ¥ 1,230 | 现货 | |
100 mg | ¥ 1,650 | 现货 | |
200 mg | ¥ 2,460 | 现货 | |
500 mg | ¥ 3,970 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 546 | 现货 |
产品描述 | Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis. |
体外活性 | 方法:人恶性黑色素瘤细胞 SK-MEL-5 和人乳腺癌细胞 MCF-7 用 Elesclomol 处理 72 h,使用 SRB 方法检测细胞活力。 结果:Elesclomol 显著抑制 SK-MEL-5 和 MCF-7 细胞生长,IC50 分别为 0.11 μM 和 0.024 μM。[1] 方法:人B淋巴细胞瘤细胞 Ramos 用 Elesclomol (500 nmol/L) 处理 24 h,使用 DCF-DA 探针监测细胞内 ROS 的水平。 结果:Elesclomol 诱导 ROS 的积累,导致荧光显微镜检测到的荧光细胞数量显著增加,较对照组细胞的 ROS 含量增加了 2.4 倍。[2] 方法:非洲绿猴肾细胞 CV-1 用 Elesclomol:Copper (70 μM) 处理 20-60 min,使用 MitoSOX 检测线粒体超氧化物。 结果:E:C 处理 20 min 诱导细胞表现出 4 倍的超氧化物生成增加。30 min 后,超氧化物水平与对照值相当。MitoSOX 荧光的减少可能是由于线粒体膜完整性的破坏和染料的损失。[3] |
体内活性 | 方法:为检测体内抗肿瘤活性,将 Elesclomol (30 mg/kg) 和 Genipin (60 mg/kg) 腹腔注射给携带人肺腺癌肿瘤 A549 的 BALB/c 小鼠,每周三次,持续四周。 结果:与对照组相比,单独用 Elesclomol 或 Genipin 治疗仅适度延缓肿瘤生长,但联合使用这两种药物可显著抑制肿瘤生长。[4] 方法:为检测对遗传性铜缺乏症 Menkes 病的治疗作用,将 Elesclomol (10 mg/kg in 2% DMSO+98%(5% methyl cellulose)) 灌胃给药给肠道特异性 Ctr1 缺失的新生小鼠,每两天一次,持续二十四天。 结果:用 Elesclomol 灌胃使肠道特异性 CTR1 敲除小鼠免于出生后早期死亡,而无需额外补充铜。[5] |
激酶实验 | In vitro enzyme assays for PLK1: Recombinant PLK1 (10 ng) is incubated with different concentrations of Rigosertib in a 15 μL reaction mixture (50 mM HEPES, 10 mM MgCl2, 1 mM EDTA, 2 mM Dithiothreitol, 0.01% NP-40 [pH 7.5]) for 30 min at room temperature. Kinase reactions are performed for 20 min at 30 °C in a volume of 20 μL (15 μL enzyme + inhibitor, 2 μL 1 mM ATP), 2 μL of γ32P-ATP (40 μCi), and 1 μL of recombinant Cdc25C (100 ng) or casein (1 μg) substrates. Reactions are terminated by boiling for 2 min in 20 μL of 2× Laemmli buffer. Phosphorylated substrates are separated by 18% SDS-PAGE. The gels are dried and exposed to X-ray film for 3-10 min. |
细胞实验 | Cells are treated with various concentrations of Elesclomol for 18 or 24 hours. The level of intracellular ROS is monitored using the DCFDA probe, which emits a green fluorescence on oxidation. Cell death is determined by flow cytometry of cells double stained with Annexin V/FITC and propidium iodide (PI) using a Vybrant Apoptosis assay kit.(Only for Reference) |
别名 | 伊利司莫, STA-4783 |
分子量 | 400.52 |
分子式 | C19H20N4O2S2 |
CAS No. | 488832-69-5 |
Smiles | CN(NC(=O)CC(=O)NN(C)C(=S)c1ccccc1)C(=S)c1ccccc1 |
密度 | 1.313 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (124.84 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 7.4 mg/mL (18.48 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. | ||||||||||||||||||||||||||||||||||||||||
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