A Nur77 antagonist
C-DIM8 is a para-phenyl-substituted diindolylmethane (C-DIM) and an antagonist of the orphan receptor nuclear receptor-related protein 77 (Nur77).1 It inhibits reporter gene expression induced by the Nur77 agonist C-DIM5 in PANC-28 cells when used at a concentration of 20 ?M. C-DIM8 (10, 15, and 20 ?M) reduces expression of BIRC5, the gene encoding survivin, in PANC-1 pancreatic cancer cells.2 In vivo, C-DIM8 (30 mg/kg) induces tumor cell apoptosis and reduces tumor volume in an L3.6pl pancreatic carcinoma mouse xenograft model.
1.Chintharlapalli, S., Burghardt, R., Papineni, S., et al.Activation of Nur77 by selected 1,1-Bis(3'-indolyl)-1-(p-substituted phenyl)methanes induces apoptosis through nuclear pathwaysJ. Biol. Chem.280(26)24903-24914(2005) 2.Lee, S.-O., Abdelrahim, M., Yoon, K., et al.Inactivation of the orphan nuclear receptor TR3/Nur77 inhibits pancreatic cancer cell and tumor growthCancer Res.70(17)6824-6836(2010)
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