PathHunter® Human CCK1 (CCKAR) Activated GPCR Internalization Cell-Based Assay Kit (U2OS)

Background Information:

The PathHunter® Human CCK1 (CCKAR) Activated GPCR Internalization Cell-Based Assay Kit (U2OS) utilizes the CCKAR Activated GPCR internalization cell line. The stable engineered cell line is designed for use in studying drug candidates (small molecules or biologics) that affect GPCR activation and internalization. This cell line enables the assessment of ligand (e.g., cholecystokinin)- based internalization of CCKAR via the 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 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.
All additional cell culture and assay reagents are available for purchase separately.

Target Class:

GPCR

Family:

Cholecystokinin

Sub Family:

Class A

Coupling:

Gq

Protein Name:

CCK1 (CCKA)

Protein Aliases:

CCK-AR|Cholecystokinin-1 receptor|CCK1-R

Accession Number:

AY322549

UniProt Number:

P32238

Gene Name:

CCKAR

Gene ID:

886

Target Species:

Human

Cell Background:

U2OS