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)
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
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M.Wt
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329.36
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Formula
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C20H15N3O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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methyl 4-(6-(pyridin-4-yl)-1H-benzo[d]imidazol-1-yl)benzoate
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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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