An orally bioavailable activator of Nurr1; selective for Nurr1 over Nur77

C-DIM12 – 100 mg

Brand:
Cayman
CAS:
178946-89-9
Storage:
-20
UN-No:
Non-Hazardous - /

C-DIM12 is a para-phenyl-substituted diindolylmethane (C-DIM) that is an orally bioavailable activator of nuclear receptor-related protein 1 (Nurr1/NR4A2).{41171} 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.{41172} 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.{41173}  

 

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Description

An orally bioavailable activator of Nurr1; selective for Nurr1 over Nur77, Nor1, and RXR; inhibits proliferation of Ku7 and 253J B-V bladder cancer cells in a dose-dependent manner at concentrations ranging from 2.5-10 µM; suppresses bladder cancer cell growth by 44 and 59% at doses of 12.5 and 25 mg/kg, respectively; neuroprotective in an MPTP mouse model of Parkinson’s disease; has analgesic and anti-inflammatory activity at a dose of 100 mg/kg in rats

Formal name: 3,3′-[(4-chlorophenyl)methylene]bis-1H-indole

Synonyms:  4-Chlorophenyl-3,3′-diindolylmethane

Molecular weight: 356.9

CAS: 178946-89-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Transcription Factors||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease||Research Area|Neuroscience|Neuroprotection||Research Area|Neuroscience|Pain Research

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