DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe[1].
DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 inhibits tau phosphorylation with an IC50 value of 0.59 μM. DYRK1-IN-1 exhibits 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 IC50 of 434 nM compared to the enzymatic IC50 of 75 nM[1].
DYRK1-IN-1 (1 mg/kg; i.v.) shows high clearance[1].
[1]. Henderson SH, et al. Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors. J Med Chem. 2021;64(15):11709-11728.