PathHunter® Human GRPR Activated GPCR Internalization Cell-Based Assay Kit (U2OS)

Background Information:

The PathHunter® Human GRPR Activated GPCR Internalization Cell-Based Assay Kit (U2OS) utilizes the GRPR Activated GPCR internalization cell line. The 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. gastrin-releasing peptide) based internalization of GRPR 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 GRPR. Upon ligand-induced receptor activation, β-arrestin 2 is recruited to the activated GPCR and the resulting GRPR-arrestin complex is internalized to the early endosome, leading to production of EFC signal.
This kit includes a stable engineered cell line (supplied as two vials of cryopreserved cells); cell line specific reagents for cell thawing, propagation, detachment, cryopreservation, and cell plating; and a 10‑plate detection kit required to run the assay. Assay plates and positive control for use in the assays can be purchased separately. For continued use of the cell line, additional quantities of cell culture and assay reagents are available for purchase separately.
Eurofins DiscoverX optimized Detection Reagents are required for optimal assay performance and must be used with these cell lines in accordance with the cell line license agreed to upon purchase of this cell line assay kit.

Target Class:

GPCR

Family:

Bombesin

Sub Family:

Class A

Coupling:

Gq

Protein Name:

BB2

Protein Aliases:

bombesin receptor 2

Accession Number:

NM_005314

UniProt Number:

P30550

Gene Name:

GRPR

Gene ID:

2925

Gene Aliases:

BB2|BB2R

Target Species:

Human

Cell Background:

U2OS