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ZJCK-6-46 (32) is a potential orally active DYRK1A inhibitor (IC50= 0.68 nM) with favorable CNC permeability. It downregulates tau phosphorylation and improves cognitive impairments by significantly reducing the expression of phosphorylated tau proteins and neuronal loss.
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Description | ZJCK-6-46 (32) is a potential orally active DYRK1A inhibitor (IC50= 0.68 nM) with favorable CNC permeability. It downregulates tau phosphorylation and improves cognitive impairments by significantly reducing the expression of phosphorylated tau proteins and neuronal loss. |
Targets&IC50 | DYRK3:17.48 nM, CLK1:1.68 nM, DYRK2:14.18 nM, DYRK4:401.3 nM, CLK3:38.91 nM, DYRK1A:0.68 nM, CLK4:1.80 nM, DYRK1B:1.02 nM |
In vivo | ZJCK-6-46 (32, 20-30 mg/kg, orally, OA-induced (MOD) mice) significantly reduces the expression of p-Tau thr212 in the CA1 and DG regions of mice induced by OA (Okadaic acid). |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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