C-DIM5

C-DIM5 is a para-phenyl-substituted diindolylmethane (C-DIM) and an agonist of the orphan receptor nuclear receptor-related protein 77 (Nur77).¹ It selectively activates Nur77 over peroxisome proliferator receptor γ (PPARγ) in reporter assays when used at a concentration of 20 μM. C-DIM5 (10, 15, and 20 μM) inhibits growth of and induces apoptosis in L3.6pL pancreatic cancer cells.² It stabilizes nuclear localization of Nur77 and Nurr1 and reduces secretion of the pro-inflammatory cytokines IL-2, IL-6, IL-12p70, CCL2, and CCL5 in primary mouse astrocytes.³ Oral administration of C-DIM5 (50 mg/kg) prevents loss of dopaminergic neurons in the substantia nigra pars compacta and striatal dopamine terminals in a mouse model of Parkinson's disease induced by MPTP.⁴

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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 pathways. The Journal of Biological Chemisty 280(26), 24903-24914 (2005).

2. Yoon, K., Lee, S.O., Cho, S.D., et al. Activation of nuclear TR3 (NR4A1) by a diindolylmethane analog induces apoptosis and proapoptotic genes in pancreatic cancer cells and tumors. Carcinogenesis 32(6), 836-842 (2011).

3. Popichak, K.A., Hammond, S.L., Moreno, J.A., et al. Compensatory expression of Nur77 and Nurr1 regulates NF-κB-dependent inflammatory signaling in astrocytes. Mol. Pharmacol. 94(4), 1174-1186 (2018).

4. De Miranda, B.R., Miller, J.A., Hansen, R.J., et al. Neuroprotective efficacy and pharmacokinetic behavior of novel anti-inflammatory para-phenyl substituted diindolylmethanes in a mouse model of Parkinson’s disease. J. Pharmacol. Exp. Ther. 345(1), 125-138 (2013).