KinaseSeeker™
Technology

Features & Benefits

  • Binding Assay: Identify active site directed as well as allosteric inhibitors
  • Luminescence detection: Low false positives from fluorescent compounds
  • Homogeneous: Portable; Adaptable to high-throughput
  • Sensitive: Low Background; Broad dynamic range

Available Screening Options

  • Inhibition at single inhibitor dose
  • Dose Response Titrations – IC50 Determinations
  • Compound Library Screening
  • Custom Assay Development

References

  1. Jester, B.W.; Cox, K.J.; Gaj, A.; Shomin, C.D.; Porter, J.R.; Ghosh, I. A Coiled-Coil Enabled Split-Luciferase Three-Hybrid System: Applied Toward Profiling Inhibitors of Protein Kinases.  Am. Chem. Soc.  2010, 132, 11727-11735.
  2. Jester, B.W.; Gaj, A.; Shomin, C.D.; Cox, K.J.; Ghosh, I. Testing the Promiscuity of Commercial Kinase Inhibitors Against the AGC Kinase Group Using a Split-luciferase Screen.  Med. Chem.  2012, 55, 1526-1537.

Protein kinases play a fundamental role in human biology, controlling many cellular processes through protein phosphorylation. Dysregulation of kinase function leads to diseases like cancer, inflammation and diabetes. Kinases are very similar in their active site architecture, which leads to cross-reactivity amongst kinase targeted small-molecule inhibitors. It is important to determine the affinity and selectivity of kinase inhibitors to minimize off-target effects while optimizing desired selectivity profiles.

KinaseSeeker™ Technology

Luceome’s kinase assay technology (KinaseSeeker™) utilizes a three-hybrid split-luciferase fragment complementation, where the reassembly of a functional luciferase from its fragments is mediated by a kinase targeted CID-probe. The luciferase reassembly results in luminescence upon addition of luciferin substrate. In Luceome’s proprietary KinaseSeeker™ assay, the competitive displacement of the CID-probe by a kinase inhibitor is measured by a change in luminescent signal. Luminescence readout translates into a highly sensitive and robust assay with low background and minimal interference from test compounds.

KinaseSeeker Assay

Luceome offers a range of cell-free and cell-based kinase assays using the KinaseSeeker technology. Use of the two formats allows comparison of compound inhibition between in vitro and cellular systems. KinaseSeeker Profiling can report on compound selectivity across different kinase groups.

Learn more about our Cell-free KinaseSeeker assays.

Learn more about our Cell-based KinaseSeeker-TE assays.

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