| 产品描述: | 胆碱激酶抑制剂;Choline kinase Inhibitors;;InformationEB-3D EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.TargetsChoKα1 (Cell-free assay) 1 μM |
| 靶点: |
IC50: 1 μM; Kd: 0.7 μM |
| 体内研究: |
EB-3D (1 mg/kg;腹腔注射;每隔一天) 在同源原位 E0771-C57BL/6 小鼠模型中抑制乳腺肿瘤的生长。 EB-3D (2.5 mg /kg;每隔一天,持续 4 周) 显示自发性肺大转移和微转移的数量减少。 |
| 参考文献: |
1. Mariotto E, et al. EB-3D a novel choline kinase inhibitor induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. Biochem Pharmacol. 2018 Sep;155:213-223. 2. Sola-Leyva A, et al. Choline kinase inhibitors EB-3D and EB-3P interferes with lipid homeostasis in HepG2 cells. Sci Rep. 2019 Mar 25;9(1):5109. 3. Schiaffino-Ortega S, et al. Design, synthesis, crystallization and biological evaluation of new symmetrical biscationic compounds as selective inhibitors of human Choline Kinase α1 (ChoKα1). 4. Mariotto E, et al. Choline Kinase Alpha Inhibition by EB-3D Triggers Cellular Senescence, Reduces Tumor Growth and Metastatic Dissemination in Breast Cancer. Cancers (Basel). 2018;10(10):391. Published 2018 Oct 22. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.552 ml |
7.759 ml |
15.517 ml |
| 5 mM |
0.31 ml |
1.552 ml |
3.103 ml |
| 10 mM |
0.155 ml |
0.776 ml |
1.552 ml |
| 50 mM |
0.031 ml |
0.155 ml |
0.31 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |