C-DIM12

C-DIM12 is a para-phenyl-substituted diindolylmethane (C-DIM) that is an orally bioavailable activator of nuclear receptor-related protein 1 (Nurr1/NR4A2).¹ It is selective for Nurr1, not activating Nur77, neuron-derived orphan receptor 1 (Nor1), or the retinoid X receptor (RXR) in parallel luciferase assays. C-DIM12 (2.5-10 µM) inhibits proliferation of Ku7 and 253J B-V bladder cancer cells in a dose-dependent manner and induces apoptosis of KU7 cells in a Nurr1-dependent manner. In an orthotopic nude mouse model, C-DIM12 suppresses bladder cancer cell growth by 44 and 59% at doses of 12.5 and 25 mg/kg, respectively. C-DIM12 has neuroprotective properties, preventing dopaminergic cell loss and reducing the expression of NF-κB in the substantia nigra pars compacta in an MPTP mouse model of Parkinson’s disease.² It also has analgesic and anti-inflammatory activity in the tail immersion and carrageenan paw edema assays at a dose of 100 mg/kg, without causing ulcers in rats.³

WARNING This product is not for human or veterinary use.

1. Inamoto, T., Papineni, S., Chintharlapalli, S., et al. 1,1-Bis(3'-indolyl)-1-(p-chlorophenyl)methane activates the orphan nuclear receptor Nurr1 and inhibits bladder cancer growth. Mol. Cancer Ther. 7(12), 3825-3833 (2008).

2. De Miranda, B.R., Popichak, K.A., Hammond, S.L., et al. Novel para-phenyl substituted diindolylmethanes protect against MPTP neurotoxicity and suppress glial activation in a mouse model of Parkinson’s disease. Toxicol. Sci. 143(2), 360-373 (2015).

3. Sujatha, K., Perumal, P.T., Muralidharan, D., et al. Synthesis, analgesic and anti-inflammatory activities of bis(indolyl)methanes. Indian J. Chem. 48B(02), 267-272 (2009).