G protein-coupled receptor kinases (GRK2) belongs to the GRK family that includes seven known GRKs, termed as GRK1-7. It is also known as β-adrenergic receptor kinase-1 (β-ARK1) and ADRBK1. It regulates the activity of G protein-coupled receptors (GPCRs). GRKs facilitate the uncoupling of GPCRs from G proteins, and participate directly in receptor endocytosis and trafficking, and modulation of ERK/MAPK cascade by GPCRs. It phosphorylates the activated form of the β2-adrenergic receptor (β2-AR) and related GPCRs. The GRK2 activity is regulated by different mechanisms including phosphorylation by kinases such as PKC, Src, ERK1/2 and p38MAPK. Phosphorylated ERK inactivates GRK2 on Ser670 in a negative feedback mechanism.

Synthetic peptide corresponding to amino acids 674-689 located at the C-terminus of human GRK2/βARK1, conjugated to KLH. The immunizing sequence is specific to GRK2 (not found in human GRK1, and GRK3-7). It is identical in dog GRK2 and highly conserved (single amino acid substitution) in rat, mouse, and bovine GRK2/βARK1.

Anti-GRK2 antibody is suitable for western blots of cortical synaptoneurosomes to study the β-arrestin-1 and ERK protein expression. It is also suitable for western blot at a concentration of 0.5-1μg/mL using HEK-293T cells expressing human GRK2 or Jurkat cell lysate.

G protein-coupled receptor kinase 2 (GRK2) is involved in the pathogenesis of chronic heart failure.

Solution in 0.01 M phosphate buffered saline, pH 7.4, containing 15 mM sodium azide.

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