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 exhibits good permeability and cellular activity without P-glycoprotein liability that can be used for the research of central nervous system penetrant DYRK1A chemical probe [1].

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 shows good permeability and cellular activity without P-glycoprotein liability. DYRK1-IN-1 has good physicochemical properties and has demonstrated high levels of enzymatic potency, favorable aqueous solubility, exquisite kinome selectivity, and promising on-target in vitro inhibition. DYRK1-IN-1 (HEK293 cells) demonstrates acceptable cellular activity, with IC 50 of 434 nM compared to the enzymatic IC 50 of 75 nM [1].

DYRK1-IN-1 (1 mg/kg; i.v.) has high clearance [1]. Animal Model: Sprague Dawley rats [1] Dosage: 1 mg/kg (Pharmacokinetic Analysis) Administration: I.v. Result: High clearance was observed.