DYR219 | DYRK1 inhibitor | Probechem Biochemicals

Chemical Structure : DYR219

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DYR219 (DYR-219)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	329.36
分子式	C20H15N3O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	methyl 4-(6-(pyridin-4-yl)-1H-benzo[d]imidazol-1-yl)benzoate

参考文献

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.

DYR219 (DYR-219)

生物&药学活性

物理化学性质&存储条件

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DYR219 (DYR-219)

生物&药学活性

物理化学性质&存储条件

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