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DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC 50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.
IC50& Target:DYRK1A 220 nM (IC 50 ) DYRK1A 3 nM (Kd) DYRK1B 56 nM (Kd)
In Vitro:DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC 50 value of 220 nM. DYRK1-IN-1 inhibits tau phosphorylation with an IC 50 value of 0.59 μM. DYRK1-IN-1 exhibits good permeability and cellular activity without P-glycoprotein liability. DYRK1-
In Vivo:DYRK1-IN-1 (1mg/kg; i.v.) shows high clearance. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague−Dawley ratsDosage: 1mg/kg (Pharmacokinetic Analysis) Administration: I.v. Res
Biological Activity:DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC 50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.