DiscoverX PathHunter™ CCKAR Activated GPCR Internalization U2OS Cell Line

The PathHunter™ CCKAR Activated GPCR internalization cell line is a stable, engineered cell line for use in studying drug candidates (small molecules or biologics) affecting GPCR activation and internalization. This cell line enables assessment of ligand (e.g. cholecystokinin) based internalization of CCKAR via detection of localization to the early endosome. This product uses EFC technology. The included cell line overexpresses EA-tagged β-arrestin 2 as well as a PK-tagged early endosome protein and untagged CCKAR. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting CCKAR-arrestin complex is internalized to the early endosome, leading to production of EFC signal. This stable modified cell line is provided as two vials of cryopreserved cells.