G protein-coupled receptor kinase 6, also known as G protein-coupled receptor kinase GRK6, GRK6 and GPRK6, is a lipid-anchor protein which belongs to the protein kinase superfamily, AGC Ser/Thr protein kinase family and GPRK subfamily. GRK6 / GPRK6 contains one AGC-kinase C-terminal domain, one protein kinase domain and one RGS domain. This protein phosphorylates the activated forms of G protein-coupled receptors thus initiating their deactivation. Several transcript variants encoding different isoforms have been described. GRK6 / GPRK6 is widely expressed. GRK6 / GPRK6 silencing causes suppression of signal transducer and activator of transcription 3 (STAT3) phosphorylation associated with reduction in MCL1 levels and phosphorylation, illustrating a potent mechanism for the cytotoxicity of GRK6 inhibition in multiple myeloma (MM) tumor cells. GRK6 also appears to be involved in responses to morphine. Inhibition of GRK6 represents a uniquely targeted novel therapeutic strategy in human multiple myeloma.
Product Name:
Human GRK6/GPRK6 Recombinant Protein (RPES2620)
Product Code:
RPES2620
Size:
20µg
Species:
Human
Expressed Host:
Baculovirus-Insect Cells
Synonyms:
GPRK6
Accession:
P43250-2
Sequence:
Met 1-Arg 589
Fusion tag:
N-His & GST
Activity:
The specific activity was determined to be 7 nmol/min/mg using casein as substrate.
Endotoxin:
<1.0 EU per µg as determined by the LAL method.
Protein Construction:
A DNA sequence encoding the human GRK6 isofrom B (P43250-2) (Met 1-Arg 589) was fused with the N-terminal polyhistidine-tagged GST tag at the N-terminus.