mProX™ Human GRK2 Stable Cell Line

Sub Cat	Product Name	Target Protein Species	Host Cell Type	Assay Types	Inquiry	Datasheet
S01YF-1122-KX1034	Magic™ Human BARK1(ADRBK1) in Vitro Assay	Human		Kinase Assay

Product Information

Target Protein

GRK2

Target Family

Kinases/Enzyme Drug Discovery Assays and Products

Target Protein Species

Human

Host Cell Type

UW228-2; CHO-K1; HEK293

Target Classification

Kinase Cell Lines

Target Research Area

Reproductive Research

Related Diseases

Asphyxiating Thoracic Dystrophy and Short-Rib Thoracic Dysplasia 1 With Or Without Polydactyly. Among its related pathways are Calmodulin induced events and Thromboxane A2 receptor signaling

Gene ID

156

UniProt ID

P25098

Product Properties

Biosafety Level

Level 1

Activity

Yes

Quantity

10⁶ cells per vial

Applications

Humans have an enzyme called G-protein-coupled receptor kinase 2 (GRK2), which is produced by the ADRBK1 gene. In order to facilitate the binding of an arrestin protein to the receptor, G protein-coupled receptor kinases phosphorylate active G protein-coupled receptors. By preventing receptor stimulation of heterotrimeric G protein transducer proteins, arrestin binding to phosphorylated, active receptors blocks their cellular signaling and causes receptor desensitization. Additionally, when an arrestin binds to a receptor, the receptor is guided into particular cellular internalization pathways, which eliminates the receptor from the cell surface and stops further activation. Receptor signaling via arrestin partner proteins is also made possible by arrestin binding to phosphorylated, active receptors. Consequently, the G protein-coupled receptors' complicated signaling switch is provided by the GRK/arrestin system. The customized GRK2 stable cell line can be used in antibody discovery and development, potential drug candidate screening and signaling pathway researches.

Protocols

Please visit our protocols page.

Customer Reviews

chat Rae

This GRK2 cell line saved us time and resources. Plus, the technical support from the company was outstanding-prompt and helpful. Dec 28 2022

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chat Natalie

This GRK2 cell line enabled us to conduct our experiments with confidence, and we achieved publication-worthy data. Mar 22 2023

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FAQ

Any questions about our products? Please visit our frequently asked questions page.

Published Data

Fig.1 GRK2 knockdown slows growth and proliferation of UW228 and Daoy medulloblastoma cell lines.

Human GRK2 knockdown miRE cassettes were introduced into Tva-expressing UW228 cells using the viruses pRDAV-m.The three options are: control pRDAV-mCherry-miRE.Ren.713 (miRE.Ren; miRE.Ctrl), Cherry-miRE.GRK2.2441 (miRE.2441), or pRDAV-mCherry-miRE.GRK2.3441 (miRE.3441).

Ref: Pathania, Anup S., et al. "GRK2 promotes growth of medulloblastoma cells and protects them from chemotherapy-induced apoptosis." Scientific Reports 9.1 (2019): 13902.

Pubmed: 31554835

DOI: 10.1038/s41598-019-50157-5

Research Highlights

One important member of the G protein-coupled receptor kinase (GRK) family is G protein-coupled receptor kinase 2 (GRK2). The plekstrin homology domain found in GRK2's C-terminus and the RGS homology domain found in GRK2's N-terminus, which has binding sites for a number of proteins and lipids, control GRK2 activity.
Han, Chen-Chen, et al. "Regulatory effects of GRK2 on GPCRs and non-GPCRs and possible use as a drug target." International Journal of Molecular Medicine 38.4 (2016): 987-994.
Pubmed: 27573285 DOI: 10.3892/ijmm.2016.2720

Identification of the GRK2-interacting proteins and substrates involved in this kinase's engagement in various cellular processes and pathological situations is being aided by an improved understanding of the GRK2 interactome and its regulation mechanisms.
Penela, Petronila, et al. "G protein-coupled receptor kinase 2 (GRK2) as a multifunctional signaling hub." Cellular and Molecular Life Sciences 76 (2019): 4423-4446.
Pubmed: 31432234 DOI: 10.1007/s00018-019-03274-3