Generic peptide substrate for use in TR-FRET biochemical kinase assays. Refer to Selector Guide for validated kinases. ULight™-labeled synthetic peptide derived from residues 463-480 of human RAC-alpha serine/threonine-protein kinase (AKT1 or PKB). AKT/PKB can be phosphorylated at Ser473 by the mTOR/Rictor complex and MAPKAP kinase 2. Peptide sequence: CSERRPHFPQFSYSASGTAR
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LANCE Ultra TR-FRET technology provides a two-component kinase assay that combines direct labeling of the kinase substrate with ULight™, an innovative emission dye for optimum binding efficiency, reducing steps and assay prep time. Validated for over 310 kinases, we provide data transparency by supplying:
For ULight substrates:
In LANCE Ultra kinase assays, the binding of a Eu-labeled anti-phosphosubstrate antibody to the phosphorylated ULight-labeled substrate brings donor and acceptor molecules into close proximity. After irradiation of the kinase reaction at 320 or 340 nm, the energy from the Eu donor is transferred to the ULight acceptor dye, which in turn generates light at 665 nm. The intensity of the light emission is proportional to the level of ULight-substrate phosphorylation.
|Detection Method||Time-Resolved Fluorescence (TRF), TR-FRET|
|Experimental Type||In vitro|
|Product Brand Name||LANCE Ultra|
|Shipping Condition||Dry Ice|
|Unit Size||5 nmol|
Protein kinases play a major role in normal cellular functions such as cell proliferation, angiogenesis, and cell adhesion. Dysregulation of kinase activity has been shown to be associated with several human diseases including cancer, diabetes and morphological disorders. This makes kinases crucial targets for the discovery and development of new drugs.
Dysregulation of kinase activity has been shown to be associated with several human diseases including cancer, diabetes and morphological disorders. Because of their function, kinases are crucial targets for drug discovery. Analysis of the human genomehas revealed the existence ofnearly 520 genes encoding kinases.
LANCE® Ultra is a high through putscreening (HTS) technology platform optimized for homogeneous time-resolved fluorescence resonance energy transfer (TRFRET) kinase assays. The LANCEUltra donor dye is a Europium(Eu) chelate, and the acceptor dye is a proprietary small-molecular weight molecule called ULight™, a fluorescent dye with a red-shifted light emission.
LANCE® Ultra TR-FRET reagents comprise the widest portfolio of validated kinase assay offerings available for rapid, sensitive ,and robust screening of purified kinase targets in a biochemical format.
Protein tyrosine kinases (PTK) are involved in the regulation of many aspects of the cell cycle, including proliferation, differentiation, secretion and apoptosis. Aberrant protein kinase expression or function is a cause or consequence of many human diseases like cancer and atherosclerosis. As a result, kinases became very important targets in drug discovery.
Of the 518 known human kinases, 90 are tyrosine (Tyr) kinases. Protein Tyr kinases play a key role in signal transduction and normal cell growth. They are also involved in numerous proliferative diseases like cancer and atherosclerosis, in addition to a number of autoimmune diseases. For these reasons, Tyr kinases are often targets for new drug discovery in many laboratories involved in basic R&D, disease and therapeutics research, and HTS.
LANCE® Ultra time-resolved fluorescence resonance energy transfer (TR-FRET) assays use a proprietary europium chelatedonor dye, W-1024 (Eu), with ULight, an innovative small molecular weight acceptor dye with a red-shifted fluorescent emission.