DUB Assays

DUB Assays

FLEXYTE™ assays harness the power and potential of fluorescence lifetime technology for screening and profiling applications:

 

  • Assays available for a range of drug target classes:
  • Robust and reliable performance
  • Homogeneous and antibody free
  • Minimises interference from problem compounds
  • Applicable to fragment based screening

FLEXYTE™ Isopeptide DUB assays

  • FLEXYTE™ FLT DUB assay platform uses full length isopeptide-linked Ub substrates to determine DUB activity
  • Ub is generated with the 9AA fluorescence lifetime reporter site-specifically attached to the C-terminus of the protein via a lysine isopeptide bond
  • A known FLT modulator, M, is incorporated at a selected site within the Ub domain modulating the lifetime of 9AA in the substrate
  • Cleavage of the physiologically-relevant Ub substrate by DUBs is directly reported through a change in the fluorescence lifetime
  • USP catalysed cleavage of the C-terminal isopeptide bond of Ub is reported through increases in the measured FLT
  • IC50 values for known inhibitors in good agreement with those reported in the literature
  • Excellent Z’-factors demonstrate the assay’s suitability for HTS applications
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