GRK5 Protein, Human (Inactive, sf9, His, GST)

GRK5 Protein, Human (Inactive, sf9, His, GST) is the recombinant human-derived GRK5 protein, expressed by Sf9 insect cells, with N-His & N-GST tag.

GRK5 is a serine/threonine kinase that preferentially phosphorylates the activated forms of various G-protein-coupled receptors (GPCRs). This receptor phosphorylation initiates β-arrestin-mediated receptor desensitization, internalization, and signaling events, leading to their down-regulation. GRK5 phosphorylates multiple GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (specifically Gi-coupled M2/M4 subtypes), dopamine receptors, and opioid receptors. Additionally, GRK5 phosphorylates other substrates such as 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)) leads to nuclear export of HDAC5, allowing MEF2-mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates the internalization of chemokine receptors. GRK5 also phosphorylates rhodopsin (RHO) (in vitro) and the non-G-protein-coupled receptor LRP6 during Wnt signaling (in vitro).

Inactive

Human

Sf9 insect cells

N-His;N-GST

P34947 (E2-S590)

2869

Partial

Approximately 95.4 kDa

Greater than 90% as determined by reducing SDS-PAGE

Solution

Supplied as a 0.2 μm filtered solution of 50 mM HEPES, pH 7.5, 200 mM NaCl, 20% glycerol, 1 mM DTT.

<1 EU/μg, determined by LAL method.

Please use rapid thawing with running water to thaw the protein.

Stored at -80°C for 1 year from date of receipt. It is stable at -20°C for 3 months after opening. It is recommended to freeze aliquots at -80°C for extended storage. Avoid repeated freeze-thaw cycles.

Shipping with dry ice.