DiscoverX PathHunter™ eXpress CCR5 Activated GPCR Internalization Assay

The PathHunter™ CCR5 Activated GPCR internalization eXpress kit provides an easy to-use cell based assay to study drug candidates (small molecules or biologics) affecting GPCR activation and internalization. This kit assesses ligand (e.g. CCL3/MIP-1α) based internalization of CCR5 via detection of localization to the early endosome. This product uses EFC technology. The included cells overexpress EA-tagged β-arrestin 2 as well as a PK-tagged early endosome protein and untagged CCR5. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting CCR5-arrestin complex is internalized to the early endosome, leading to production of EFC signal. eXpress kits are a convenient, ready-to-use format which contains all materials needed to run the assay, including single-use vials of cryopreserved cells, cell plating media, detection reagent, and assay plates.