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Recombinant GRK5 protein
| Aliases: G-protein Receptor Kinase 5 |
| Catalog No: 81382 | Format: 20 µg | ¥3,840 | Add to Cart |
| Catalog No: 81682 | Format: 1 mg | ¥33,200 | Add to Cart |
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Expressed In: Baculovirus Protein Species: Human
Contents
A representative Technical Data Sheet (TDS) is provided here. Please refer to the lot-specific TDS you will receive with your order for the lot-specific buffer contents and protein concentration.
Background
GRK5 is a serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein-coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. GRK5 phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, it also phosphorylates various substrates: Hsc70-interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2-mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates internalization of the chemokine receptor. Diseases associated with GRK5 include Systolic Heart Failure and Palmoplantar Keratoderma and Congenital Alopecia 2.
Application Notes
This product was manufactured as described in Protein Details. Where possible, Active Motif has developed functional or activity assays for recombinant proteins. Additional characterization such as enzyme kinetic activity assays, inhibitor screening or other biological activity assays may not have been performed for every product. All available data for a given product is shown on the lot-specific Technical Data Sheet.
Protein Details
Recombinant GRK5 protein was expressed in baculovirus expression system as the full length protein (accession number NP_005299.1) with a N-terminal FLAG tag. The molecular weight of the protein is 68.8 kDa.
References
Human
Recombinant GRK5 protein
10% SDS-PAGE with Coomassie staining
MW: 68.8 kDa
Purity: >50%
HTRF assay for GRK5 activity
1 µM STK S3 substrate was incubated with different concentrations of GRK5 protein in a 10 µl reaction system containing 1×Enzymatic Buffer, 5 mM MgCl2, 2 mg/ml Casein, 1 mM DTT and 100 µM ATP for 1 hour. Then 10 µl detection reagents containing STK antibody (1:2) and SA-XL665 (1:100) diluted with 1× Detection Buffer were added and incubated with the reactions for 30 min. All the operations and reactions were performed at room temperature. HTRF assay was used for detection
Storage
Recombinant proteins in solution are temperature sensitive and must be stored at -80°C to prevent degradation. Avoid repeated freeze/thaw cycles and keep on ice when not in storage.
Guarantee
This product is guaranteed for 6 months from date of arrival.
