| Description | DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. |
| In vitro | DIM-C-pPhCO2Me抑制了ACHN和786-O细胞的生长并诱导了凋亡[1]。DIM-C-pPhCO2Me降低了RMS细胞中NR4A1依赖的转激活作用，并抑制了RMS细胞和肿瘤的生长，诱导了凋亡。NR4A1的敲除和DIM-C-pPhCO2Me的处理均诱导了ROS产生，这激活了应激基因并诱导了sestrin 2的产生，后者激活了AMPK并抑制了突变型p53 RMS细胞中的mTOR[2]。 |
| Cell experiments | 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 [1]. |
| molecular weight | 380.44 |
| Molecular formula | C25H20N2O2 |
| CAS | 151358-48-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (131.43 mM) |
| References | 1. Hedrick E, et al. Nuclear Receptor 4A1 (NR4A1) as a Drug Target for Renal Cell Adenocarcinoma. PLoS One. 2015 Jun 2;10(6):e20128308. 2. Lacey A, et al. Nuclear receptor 4A1 (NR4A1) as a drug target for treating rhabdomyosarcoma (RMS). Oncotarget. 2016 May 24;7(21):31257-69. |