| 产品描述: | ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis. |
| 体内研究: |
ARN5187 trihydrochloride (compound 1) (0-100 µM; 48 h) shows cytotoxicity with EC50 of 23.5 µM in BT-474 cells and IC50 of 30.14 µM, >100 µM for BT-474 and HMEC cells, respectively. ARN5187 trihydrochloride (0-100 µM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells. ARN5187 trihydrochloride (25, 50 µM) is a lysosomotropic-independent REV-ERB antagonistic activity. ARN5187 trihydrochloride (50 µM; 24 h) shows autophagy inhibition. ARN5187 trihydrochloride (50 µM; 2, 8, 24 h) effects autophagy formation and maturation. |
| 保存条件: |
-80°C 12个月; -20°C 6个月, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.973 ml |
9.864 ml |
19.727 ml |
| 5 mM |
0.395 ml |
1.973 ml |
3.945 ml |
| 10 mM |
0.197 ml |
0.986 ml |
1.973 ml |
| 50 mM |
0.039 ml |
0.197 ml |
0.395 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。 |