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DYR219

Chemical Structure : DYR219

CAS No.: 2088422-05-1

DYR219 (DYR-219)

Catalog No.: PC-23234Not For Human Use, Lab Use Only.

DYR219 is a potent, selective, type 1 ATP-competitive inhibitor of DYRK1 with IC50 of 34 nM (DYRK1A) and 29 nM (DYRK1B), induces degradation of Dyrk1a protein.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    DYR219 is a potent, selective, type 1 ATP-competitive inhibitor of DYRK1 with IC50 of 34 nM (DYRK1A) and 29 nM (DYRK1B), induces degradation of Dyrk1a protein.
    DYR219 inhibited Dyrk1a catalyzed tau phosphorylation at the pS396 epitope (IC50 = 127 nM; [ATP] = 1 mM).
    DYR219 inhibited tau protein phosphorylation at the pS396 epitope with an EC50 of 142 nM in H4 neuroglioma cells expressing 4R0N tau.
    DYR219 caused a significant reduction of DYRK1A protein levels by an unknown mechanism, an effect that likely contributes to its in vivo efficacy in a mouse model of Alzheimer's disease.

    Physicochemical Properties

    M.Wt 329.36
    Formula C20H15N3O2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    methyl 4-(6-(pyridin-4-yl)-1H-benzo[d]imidazol-1-yl)benzoate

    References

    1. Velazquez R, et al. Mol Neurobiol. 2019 Dec;56(12):8364-8375.

    2. Zhu B, et al. Sci Rep. 2022 Sep 23;12(1):15847.

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