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.

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]

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]

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.

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)