In-Cell KinaseScreen Services

Protein kinases are key regulators of many critical cellular processes including cell cycle, proliferation, metabolism, differentiation, and apoptosis. More than 500 protein kinases are identified in human representing approximately 2% of the genome. Kinase dysfunction has been implicated in a variety of human diseases including cancer, diabetes, cardiovascular and neurological diseases, psoriasis, asthma, and rheumatoid arthritis. As a result, protein kinases are now considered to be the second most important group of drug targets and represent an important target class to consider for potential drug liability issues. Protein kinase inhibitors are important not only for their therapeutic properties, but also as invaluable research tools to study cell signaling. 

Biochemical-based kinase assays are important tools to assist researchers in accelerating their lead identification and optimization efforts while reducing the costs. However, it is pivotal to confirm the drug/target inhibition and selectivity in a more physiologically relevant cellular environment to limit the chances of false positive or negative data in early stages of drug development.

Caliper Discovery Alliances & Services (CDAS) In-Cell KinaseScreen provides reliable, quantitative means for determining the specific drug effects on the kinase targets of interest in a more physiologically relevant cellular environment. This allows for a more predictive characterization of the organism’s physiological response to the drug. Our In-Cell KinaseScreen assays offer complete molecular screening of 10 kinase targets in addition to custom assay development.

Technology Platform

CDAS In-Cell KinaseScreen is an antibody-based flow cytometry system with the unique ability to accurately determine “kinase activation” and “kinase activity” in a relevant cell model. This allows us to measure the effect of the activated kinase of interest on its immediate and specific downstream target protein (substrate) in the presence of the drug. In addition, our assays target an epitope on the target protein that gets specifically phosphorylated by the upstream kinase of interest which makes the obtained results even more selective and reliable. This enables us to distinguish between different upstream effectors and to specifically study the pathway of interest.

List of In-Cell KinaseScreen Assays

The following table is a listing including, but not limited to, the kinase targets in our platform. Our assays can be designed and customized against different kinases and target proteins according to the clients’ specific needs.

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In-Cell KinaseScreen Services

In-Cell KinaseScreen Profiling and Screening

• Panel of 10 In-Cell Kinase Assays
• Confirm drug specificity for the kinase target or identify new kinase targets
• Low to high throughput compound screening

In-Cell KinaseScreen IC₅₀

• Determine drug inhibitor potency in selected kinase assay
• Compare your drug profile with reference compound inhibitor

Custom Assay Development

• Any targets/pathways
• Wide choice of cell hosts available
• Multiplex options available

In-Cell KinaseScreen Complementary Services

• In vitro and in vivo drug safety assessments
• Drug monotherapy and combination studies in selected cancer cell lines
• Cancer cell line profiling (200+ human cell lines in-house)
• Drug efficacy testing in relevant animal models

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In-Cell KinaseScreen Key Applications and Benefits:

• Signal Transduction and Drug Development Research
• Drug Screening Assays and Selectivity Profiiling
• Full Evaluation of the Drug Effects, Pathway Idenfiication and Analysis 
• Complement to Conventional Drug Safery Data

• Customizable (choice of kinase, target protein, specific eptope, antibody, cell host, etc.)
• More than 200 Fully Characterized Non-Recombinant Human Cell Lines with Endogenous Expression of Effector Kinase
• Multiplexable (assessment of multiple targets in an entire pathway or multiple pathways)
• Multiple Levels of Assay Specificity
• Specific Pathway Stimulation using Selective Inducers
• Versatile (low to high throughput, predefined or customized assays)
• Robust and Reproducible Results
• Rapid Turnaround Time