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Human GRK6 / GPRK6 Protein (His & GST Tag)

GPRK6

Catalog Number P11752-H20B
Organism Species Human
Host Baculovirus-Insect Cells
Synonyms GPRK6
Molecular Weight The recombinant human GRK6/GST chimera consists of 826 amino acids and has a calculated molecular mass of 95.1 kDa. It migrates as an approximately 85 kDa band in SDS-PAGE under reducing conditions.
predicted N Met
SDS-PAGE
Purity > 93 % as determined by SDS-PAGE
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.
Bio-activity The specific activity was determined to be 7 nmol/min/mg using casein as substrate.
Research Area Signaling |Signal Transduction |G protein signaling |Heterotrimeric G Proteins |GPCR Kinases
Formulation Supplied as sterile 20mM Tris, 500mM NaCl, 2mM GSH, 0.5mM PMSF, pH 7.4
1. Normally 5 % - 8 % trehalose, mannitol and 0.01% Tween80 are added as protectants before lyophilization. Specific concentrations are included in the hardcopy of COA.
Background 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.
Reference
  • Ghadessy,R.S. et al., 2003, Br J Pharmacol  138 (4):660-70.
  • Murga,C. et al., 2009, Brain Behav Immun. 23 (1):16-7.
  • Tiedemann,R.E. et al., 2010, Blood  115 (8):1594-604.
  • Ahmed,M.R. et al., 2010, Sci Transl Med 2 (28): 28ra28.