C-DIM12

Catalog No.S8097 Batch:S809701

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Technical Data

Formula

C23H17ClN2
Molecular Weight 356.85 CAS No. 178946-89-9
Solubility (25°C)* In vitro DMSO 71 mg/mL (198.96 mM)
Ethanol 71 mg/mL (198.96 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].
In vivo C-DIM12 has the neuroprotective activity in MPTPp-treated mice[2].

Protocol (from reference)

Cell Assay:[2]
  • 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.
Animal Study:[1]
  • Animal Models

    Transgenic NF-κB/EGFP reporter mice (C57Bl/6 background)

  • Dosages

    50 mg/kg

  • Administration

    oral administration

Selleck's C-DIM12 has been cited by 2 publications

α-Synuclein Negatively Regulates Nurr1 Expression Through NF-κB-Related Mechanism [ Front Mol Neurosci, 2020, 23724] PubMed: 32477062
miR-381-3p knockdown improves intestinal epithelial proliferation and barrier function after intestinal ischemia/reperfusion injury by targeting nurr1. [ Cell Death Dis, 2018, 9(3):411] PubMed: 29540663

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.