C-DIM12

C-DIM12 is a Nurr1 activator that stimulates Nurr1 mediated apoptosis axis in bladder cancer cells and tumors and inhibits NF-κB–dependent gene expression in glial cells.

C-DIM12 Chemical Structure

C-DIM12 Chemical Structure

CAS No. 178946-89-9

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Biological Activity

Description C-DIM12 is a Nurr1 activator that stimulates Nurr1 mediated apoptosis axis in bladder cancer cells and tumors and inhibits NF-κB–dependent gene expression in glial cells.
Targets
Nurr1 [2]
In vitro
In vitro C-DIM12 induces Nurr1 and DA gene expression in cell lines and primary neurons[3]. C-DIM12 suppresses astrocyte inflammatory signaling in vitro. C-DIM12 inhibits lipopolysaccharide (LPS)–induced expression of NF-κB-regulated genes in BV-2 microglia including nitric oxide synthase (NOS2), interleukin-6 (IL-6), and chemokine (C-C motif) ligand 2 (CCL2), and the effects were attenuated by Nurr1-RNA interference. Additionally, C-DIM12 decreased NF-κB activation in NF-κB–GFP (green fluorescent protein) reporter cells and enhanced nuclear translocation of Nurr1 primary microglia. C-DIM12 decreases lipopolysaccharide-induced p65 binding to the NOS2 promoter and concurrently enhanced binding of Nurr1 to the p65-binding site. C-DIM12 also stabilized binding of the Corepressor for Repressor Element 1 Silencing Transcription Factor (CoREST) and the Nuclear Receptor Corepressor 2 (NCOR2)[2].
Cell Research Cell lines HEK293 cells
Concentrations 100 μM
Incubation Time 24 h
Method NF-κB–GFP HEK cells are exposed to 30 ng/ml of TNFα in the presence of 100 μM C-DIM12 for up to 24 hours. C-DIM12 is efficient at blocking NF-κB–GFP expression in the NF-κB–GFP HEK cells after TNFα treatment, displaying a statistically significant reduction in total GFP fluorescence per cell.
In Vivo
In vivo C-DIM12 has the neuroprotective activity in MPTPp-treated mice[2].
Animal Research Animal Models Transgenic NF-κB/EGFP reporter mice (C57Bl/6 background)
Dosages 50 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 356.85 Formula

C23H17ClN2

CAS No. 178946-89-9 SDF Download C-DIM12 SDF
Smiles C1=CC=C2C(=C1)C(=CN2)C(C3=CC=C(C=C3)Cl)C4=CNC5=CC=CC=C54
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 71 mg/mL ( (198.96 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 71 mg/mL

Water : Insoluble


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In vivo
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