DIM-C-pPhCO2Me is an antagonist of nuclear receptor 4A1 (NR4A1).

DIM-C-pPhCO2Me inhibited growth and induced apoptosis in ACHN and 786-O cells [1]. 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 [2].

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].