Name :
Recombinant Human GRK6 Protein (His & GST Tag)
Biological Activity :
Background :
G protein-coupled receptor kinase 6, also known as G protein-coupled receptor kinase GRK6, GRK6, and GPRK6, is a lipid-anchor protein that 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 a 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.
Biological Activity :
The specific activity was determined to be 7 nmol/min/mg using casein as substrate.
Expression Host :
Human
Source :
Baculovirus-Insect Cells
Tag :
Protein Accession No. :
P43250-2
NCBI Gene ID :
Synonyms :
Synonyms :
G protein-coupled receptor kinase 6
Amino Acid Sequence :
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.
Purity :
> 93 % as determined by SDS-PAGE
State of Matter :
Product Concentration :
Storage and Stability :
Samples are stable for up to twelve months from date of receipt at -20℃ to -80℃. Store it under sterile conditions at -20℃ to -80℃. It is recommended that the protein be aliquoted for optimal storage. Avoid repeated freeze-thaw cycles.
Endotoxin Level :
< 1.0 EU per μg of the protein 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.
Buffer Solution :
Supplied as sterile 20mM Tris, 500mM NaCl, 2mM GSH, 0.5mM PMSF, pH 7.4Please contact us for any concerns or special requirements.Please refer to the specific buffer information in the hardcopy of datasheet.
Shipping :
Kinases are highly recommended to be shipped at frozen temperature with blue ice or dry ice.Shipment made at ambient temperature may seriously affect the activity of the ordered products.
Redissolution :
A hardcopy of COA with reconstitution instruction is sent along with the products. Please refer to it for detailed information.
Synonyms :
GPRK6 Protein, Human GRK6 背景信息 G protein-coupled receptor kinase 6, also known as G protein-coupled receptor kinase GRK6, GRK6, and GPRK6, is a lipid-anchor protein that 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 a 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.
References & Citations :
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.
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