Product Description
GRK5 (G protein-coupled receptor kinase 5), also known as GPRK5, is a member of the serine/threonine protein kinase family that plays a pivotal role in homologous desensitization and internalization of G protein-coupled receptors (GPCRs), as well as in cell signaling, migration, and inflammation. GRK5 is activated by binding to activated GPCRs or through phosphorylation by protein kinase C (PKC) and interaction with membrane phospholipids (e.g., PIP2), leading to receptor phosphorylation and subsequent recruitment of β-arrestins. Beyond its role in normal cardiovascular function, neuronal signaling, and immune regulation, dysregulation of GRK5 signaling—through overexpression, genetic polymorphisms (e.g., Q41L variant), or aberrant nuclear translocation—is closely associated with heart failure, cardiac hypertrophy, Alzheimer's disease, Parkinson's disease, hypertension, and various cancers (including breast and prostate cancer), making it a highly validated target for cardiovascular therapy, neurodegenerative disease treatment, and drug discovery.
Screeningbio’s GRK5 Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying GRK5 kinase activity and evaluating the potency of tyrosine kinase inhibitors (TKIs).
This kit utilizes the ADP-Glo Kinase Assay platform, a luminescent technology that measures the amount of ADP produced during the kinase reaction.
The assay is performed in two distinct steps:
Kinase Reaction: GRK5 catalyzes the transfer of a phosphate group from ATP to a specific substrate, resulting in the production of phosphorylated substrate and ADP.
ADP-Glo™ Reagent Addition: After the kinase reaction, the ADP-Glo™ Reagent is added to terminate the reaction and deplete any remaining unreacted ATP.
Kinase Detection: The Kinase Detection Reagent is added to simultaneously convert the produced ADP back into ATP, which is then used by luciferase to generate a luminescent signal.
The light intensity produced is directly proportional to the ADP concentration and, consequently, to the enzymatic activity of the GRK5 kinase.
Data