Digitoxin 是一种有效的 Na+/K+-ATPase 抑制剂,Digitoxin 的 EC50 值为 0.78 μM。
Cas No. | 71-63-6 |
别名 | 洋地黄毒苷 |
Canonical SMILES | C[C@H]1O[C@](O[C@@H]2[C@@H](C)O[C@](O[C@H]3[C@@H](O)C[C@@](O[C@@H]4C[C@](CC[C@]5([H])[C@]6([H])CC[C@@]7(C)[C@]5(O)CC[C@@H]7C(CO8)=CC8=O)([H])[C@]6(C)CC4)([H])O[C@@H]3C)([H])C[C@@H]2O)([H])C[C@H](O)[C@@H]1O |
分子式 | C41H64O13 |
分子量 | 764.94 |
溶解度 | DMSO : ≥ 100 mg/mL (130.73 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Digitoxin is an effective Na+/K+-ATPase inhibitor, the EC50 value of Digitoxin is 0.78 μM.IC50 value: 0.78 μM (EC50)Target: Na+/K+-ATPasein vitro: Digitoxin shows a significantly cytotoxic effect in H1975 cells by causing G2 phase arrest, also remarkably activates 5’ adenosine monophosphate-activated protein kinase (AMPK). Moreover, Digitoxin suppresses microtubule formation through decreasing α-tubulin. Digitoxin effectively depresses the growth of TKI-resistance NSCLC H1975 cells by inhibiting microtubule polymerization and inducing cell cycle arrest. Digitoxin has the highest cytotoxicity in H1975 cells, whose CC50 value was 0.19 ± 0.06 μM. Digitoxin-induced inhibition mechanism is likely due to causing G2/M cell cycle arrest in H1975 cells in dose dependent manners. [1]. Zhang YZ, et al. Compound Library Screening Identified Cardiac Glycoside Digitoxin as an Effective Growth Inhibitor of Gefitinib-Resistant Non-Small Cell Lung Cancer via Downregulation of α-Tubulin and Inhibition of Microtubule Formation. Molecules. 2016 |