伊利司莫 T6170

Product Introduction
Bioactivity


英文名: Elesclomol

描述: 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。

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)

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.

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: 5% DMSO+95% Saline : 3.7 mg/mL (9.24 mM, suspension)
DMSO : 50 mg/mL (124.84 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: copper ionophore | Reactive Oxygen Species | ferredoxin 1 | ROS | hereditary copper | Elesclomol | Inhibitor | FDX1 | cancer | Menkes | Fe-S cluster | Cuproptosis | β5 strand | α2/α3 helices | STA 4783 | Apoptosis | copper | oxidative stress | STA4783 | inhibit

相关产品: Silybin B | Dinoprost tromethamine salt | Isoalantolactone | Trametinib | Torin 2 | Nystatin | Cabozantinib S-malate | Phenoxodiol | DB1976 | Sodium diatrizoate

相关库: Anti-Aging Compound Library | Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Anti-Parkinson's Disease Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Active Compound Library | Apoptosis Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途