Cellular Kinase Profiling, Screening and Assays
Tyrosine Kinase Cell-Based Assay Services
The largest commercially available panel of tyrosine kinase cell-based assays is offered in collaboration with Advanced Cellular Dynamics.
The assay principle builds on IL3-dependent Ba/F3 cells that are modified to express an activated recombinant kinase. Following removal of IL3, the modified cells are dependent on the activity of the recombinant kinase for survival and proliferation. Inhibition of the kinase activity results in a directly proportional decrease in cell viability.
The Ba/F3 cell system is a powerful tool for profiling compounds in vivo:
- Activity is measured towards physiological conformations of kinases.
- Activity of compounds that preferentially bind to inactive conformations of kinases can be measured. Kinase substrates in the Ba/F3 system are likely to be biologically relevant substrates required for cell proliferation and survival.
- Membrane penetration and potency shifts due to plasma protein binding are addressed.
- Toxicity of compounds is detected.
NanoBRET Target Engagement (TE) Intracellular Kinase Assay Service
Quantifying kinase inhibitor occupancy, selectivity, affinity within the cellular environment where engagement would naturally occur is crucial to more accurately predict its engagement potencies against human kinases. In addition to equilibrium evaluation, it’s also desirable to obtain kinetic parameters such as Residence Time for better compound optimization. Quantitative and wide-spectrum kinase profiling services using the NanoBRET™ Target Engagement Intracellular Kinase Assay System (Promega) enable you to assess your compound’s engagement for a selected intracellular target under physiological conditions, including compound Residence Time at the target while keeping the cells intact.
The NanoBRET™ Assay services comprise % inhibition, IC50 determination, and residence time analysis.
First-time customers: please contact us for a special offer!