| 产品描述: | DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. |
| 体外研究: |
DIM-C-pPhCO2Me inhibited growth and induced apoptosis in ACHN and 786-O cells. DIM-C-pPhCO2Me decreased NR4A1-dependent transactivation in RMS cells and inhibited RMS cell and tumor growth and induced apoptosis. Both NR4A1 knockdown and treatment with DIM-C-pPhCO2Me also induced ROS which activated stress genes and induced sestrin 2 which activated AMPK and inhibited mTOR in the mutant p53 RMS cells |
| 体内研究: |
Knockdown of NR4A1 in ACHN and 786-O cells was carried out using Lipofectamine 2000 reagent according to the manufacturer's protocol. siRNA complexes used in the study are as follows: siGL2-5', CGU ACG CGG AAU ACU UCG A; siNR4A1 (1)-SASI_Hs02_00333289; siNR4A1 (2)-SASI_Hs01_00182072. ACHN RCC cells were plated on 12-well plates at 5 x 104 cells per well in DMEM supplemented with 2.5% charcoal-stripped FBS. After 24 hr, various amounts of DNA [NBRE3-luc (400 ng), FLAG-NR4A1 (40 ng)] were cotransfected into each well by Lipofectamine 2000 reagent according to the manufacturer's protocol. After 6 hr of transfection, cells were treated with 2.5% stripped DMEM containing either DMSO, DIM-C-pPhOH (20 μM) or DIM-C-pPhCO2Me (15 μM) for 18 hr |
| 参考文献: |
1. Lacey A, et al. Nuclear receptor 4A1 (NR4A1) as a drug target for treating rhabdomyosarcoma (RMS). Oncotarget. 2016 May 24;7(21):31257-69. 2. Hedrick E, et al. Nuclear Receptor 4A1 (NR4A1) as a Drug Target for Renal Cell Adenocarcinoma. PLoS One. 2015 Jun 2;10(6):e20128308. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.629 ml |
13.143 ml |
26.285 ml |
| 5 mM |
0.526 ml |
2.629 ml |
5.257 ml |
| 10 mM |
0.263 ml |
1.314 ml |
2.629 ml |
| 50 mM |
0.053 ml |
0.263 ml |
0.526 ml |
|
| 注意: |
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