生物活性 | |||
---|---|---|---|
描述 | ATN-224 demonstrates a unique and robust attraction to copper ions (108 mol/L), without affinity for calcium, iron, magnesium, zinc, or manganese ions up to concentrations of 1 mM, as revealed by isothermal titration calorimetry. It restricts the growth of HUVEC (IC50=1.4±0.3 μM; n=5) and inhibits bovine SOD1 activity (IC50=0.33±0.03 μM after 24 hours). The suppression of SOD1 by ATN-224 is both time-bound, peaking around 16 hours, and dose-dependent, demonstrating an IC50 of 17.5±3.7 nM in endothelial cells. Additionally, it deters FGF-2-stimulated ERK1/2 phosphorylation correlating with its anti-proliferative IC50 range (1.25-2.5 μM)[1]. Orally administered ATN-224 targets and inhibits the copper/zinc-dependent superoxide dismutase 1 (Cu/Zn-SOD1) in endothelial and cancer cells[2]. |
实验方案 | |||
---|---|---|---|
1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.31mL 0.46mL 0.23mL |
11.56mL 2.31mL 1.16mL |
23.12mL 4.62mL 2.31mL |
参考文献 |
---|