GRK2 Protein, Human (sf9, His-GST)

The GRK2 protein is a highly specific, selective phosphorylation agonist that occupies beta-adrenergic receptors and related receptors, inducing desensitization and serving as an important regulatory mechanism. In addition to G protein-coupled receptor desensitization, GRK2 actively regulates the ciliary smoothing (SMO)-dependent Hedgehog (Hh) pathway by promoting SMO transport and enhancing SMO activity. GRK2 Protein, Human (sf9, His-GST) is the recombinant human-derived GRK2 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of GRK2 Protein, Human (sf9, His-GST) is 689 a.a., with molecular weight of ~110 kDa.

GRK2 protein demonstrates a high degree of specificity as it selectively phosphorylates the agonist-occupied form of beta-adrenergic and closely related receptors, provoking their desensitization. This phosphorylation activity serves as a pivotal regulatory mechanism in receptor signaling. Additionally, GRK2 acts as a key modulator in LPAR1 signaling, engaging in competition with RALA for LPAR1 binding and influencing the receptor's signaling properties. Notably, GRK2 exhibits a phosphorylation-independent desensitization of LPAR1 and LPAR2. Beyond its role in G protein-coupled receptor desensitization, GRK2 plays a significant positive regulatory role in the ciliary Smoothened (SMO)-dependent Hedgehog (Hh) signaling pathway by facilitating SMO trafficking into the cilium and enhancing SMO activity. Furthermore, GRK2's involvement in the regulation of airway smooth muscle relaxation in response to blue light adds another layer to its diverse functional repertoire.

Human

Sf9 insect cells

N-His;N-GST

P25098 (M1-L689)

156  [NCBI]

Approximately 110 kDa

Greater than 90% as determined by reducing SDS-PAGE

<1 EU/μg, determined by LAL method.