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    IM-12
    IM-12

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0226
    CAS #: 1129669-05-1Purity ≥98%

    Description: IM-12, an indolylmaleimide analog, is a novel, potent, cell-permeable and selective inhibitor of GSK-3β (glycogen synthase kinase-3β) with potential neuroprotective effects. It inhibits GSK-3β with an IC50 of 53 nM. Treatment of human neural progenitor cells with IM-12 resulted in an increase of neuronal cells. IM-12 acts via the canonical Wnt signalling pathway by inhibition of the key enzyme GSK-3beta. The Wnt pathway is involved in cellular processes linked to either proliferation or differentiation..

    References: Bioorg Med Chem. 2010 Sep 15;18(18):6785-95.

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    Molecular Weight (MW)

    377.41

    Formula

    C22H20FN3O2

    CAS No.

    1129669-05-1

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 75 mg/mL (198.7 mM)

    Water: <1 mg/mL

    Ethanol: 10 mg/mL (26.5 mM)

    SMILES

     FC(C=C1)=CC=C1CCNC(C2=O)=C(C(N2C)=O)C(C3=C(C=CC=C3)N4)=C4C

    Synonyms

     IM-12; IM 12; IM12; 3-(4-Fluorophenylethylamino)-1-methyl-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione


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    In Vitro

    In vitro activity: In hNPCs, IM-12 inhibits GSK-3β activity with IC50 of 3.8 μM and subsequently increases β-catenin concentration significantly. Through the activation of canonical Wnt signalling pathway, IM-12 promotes the neuronal differentiation of human neural progenitor cells.

     

    Kinase Assay: IC50 of new synthesised compound IM-12 to GSK-3β is determined by a luminometric GSK-3β activity assay. Briefly, compounds are tested in different concentrations diluted in assay buffer containing final concentrations of: 4 mM MOPS pH 7.2; 0.4 mM EDTA; 1 mM EGTA; 2.5 mM β-glycerophosphate; 4 mM MgCl2; 40 μM BSA; 0.05 mM DTT. Four microlitres of diluted compounds are added to 25 μM pGS-2 peptide substrate, 20 ng recombinant GSK-3β and 1 μM ATP to a total assay volume of 40 μl. The enzymatic reaction is stopped after 30 min of incubation at 30 °C by adding 40 μl KinaseGlo. The luminometric signal is allowed to stabilise for 10 min and the measured with a Glomax® 96 Microplate Luminometer. 

     

    Cell Assay: To measure viable cells, 50-100 μL of cell suspension is analyzed using CASY technology with the appropriate program. ReNcell VM cells are seeded at a defined cell number and proliferated for 24 h. Then the medium is changed to proliferation medium with added substances at indicated concentrations. The cell number was determined every 24 h. Cells were exposed to the added drugs during the whole experiment, whereas the media is changed every 24 h.

    In Vivo

    NA

    Animal model

    NA

    Formulation & Dosage

    NA

    References

    Bioorg Med Chem. 2010 Sep 15;18(18):6785-95.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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