Catalog No.: PC-60585Not For Human Use, Lab Use Only.
Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3 with IC50 of 18 nM and 5.4 nM, respectively.
Compound 101 (GRK2 inhibitor 101, Takeda compound 101, Cmpd101) is a novel membrane-permeable, small-molecule inhibitor of GRK2 and GRK3 with IC50 of 18 nM and 5.4 nM, respectively.
Compound 101 inhibits the desensitization of the G protein-activated inwardly-rectifying potassium current evoked by receptor-saturating concentrations of Met-Enk, DAMGO, endomorphin-2, and morphine in rat and mouse locus coeruleus neurons.
Compound 101 produces complete inhibition of DAMGO-induced MOPr phosphorylation at Ser(375), arrestin translocation, and MOPr internalization in HEK 293 cells.
