| 产品描述: | R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties. |
| 体外研究: |
Inhibition of GDH1 activity by R162 treatment results in decreased intracellular fumarate levels, attenuated GPx activity, increased ROS levels, and reduced cell proliferation in H1299 and MDA-MB231 cells, which can be significantly rescued by methyl-α-KG treatment as well as by antioxidant NAC. R162 inhibits cell proliferation and tumor growth potential of human cancer cells |
| 体内研究: |
R162 (30 mg/kg/day, i.p.) does not result in a significant histopathological change between the vehicle-treated and R162-treated groups, nor alters complete blood counts, or hematopoietic properties in xenograft tumor mouse models. R162 (20 mg/kg/day) results in significantly decreased tumor growth and masses in mice compared with control mice and effectively inhibits GDH1 activity in resected tumors from xenograft nude mice |
| 参考文献: |
1. Jin L, et al. Glutamate dehydrogenase 1 signals through antioxidant glutathione peroxidase 1 to regulate redox homeostasis and tumor growth. Cancer Cell. 2015 Feb 9;27(2):257-70. |
| 溶解性: |
Soluble in DMSO、Ethanol、DMF |
| 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 |
3.784 ml |
18.92 ml |
37.839 ml |
| 5 mM |
0.757 ml |
3.784 ml |
7.568 ml |
| 10 mM |
0.378 ml |
1.892 ml |
3.784 ml |
| 50 mM |
0.076 ml |
0.378 ml |
0.757 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。 |