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Product IntroductionBioactivity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，
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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
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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