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Kinase Product Solutions

Kinase Enzymes and Cell-Based Functional, Binding, and Activity Assays for Discovery through Development and for QC Lot-Release Testing

Kinases play a central in cell signaling to elicit many physiological responses. Dysregulation of kinase activity leads to many human diseases, especially cancer. A typical signaling pathway involves a kinase cascade to produce a cellular response starting with receptor activation via a ligand-induced activation step. Receptor-specific ligands, such as growth factors, result in receptor tyrosine kinases (RTK) dimerization or oligomerization. This often results in the receptors’ activation and autophosphorylation, allowing them to recruit and activate downstream mediators via their SH2 domains. This event then triggers a signaling cascade that leads to the phosphorylation and activation of downstream kinases to act upon various downstream target molecules, including several cytoplasmic targets and transcriptional factors. The activated targets elicit cellular responses that include the promotion of cell growth and division, protein translation, or other physiological responses.

 

Eurofins DiscoverX® offers an extensive portfolio of functional and binding cell-based assays, cell lines, and recombinant kinase enzymes to evaluate any kinase target-based signaling activities to aid your efforts from discovery through development into commercialization. Screen for novel kinase inhibitors, perform pharmacological profiling, and evaluate kinase activation from therapeutic binding. Utilize cell-based assays to determine therapeutic mechanism of action (MOA) and intracellular compound target engagement. Perform kinase activity assays measuring ADP production or substrate phosphorylation with one of the most extensive offerings of recombinant kinase enzymes available.

 

As the new home of the original Millipore (Upstate) kinase enzyme portfolio covering over >70% of the kinome combined with the clinically-proven PathHunter® MOA-reflective, cell-based assay platform, Eurofins DiscoverX has the kinase solutions you need to integrate into your discovery and development pipelines to accelerate your drug discovery programs.

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Benefits of Kinase Product Solutions

  • Comprehensive Portfolio – Binding and functional, cell-based assays for receptor dimerization, SH2 recruitment, and target engagement as well as over 420 kinases active, mutant, and inactive recombinant kinases for activity and biophysical testing
  • Highly Applicable – Ideal for the development of small molecule and biologic therapeutics, from target ID through pre-clinical drug development programs, into therapeutic commercial release
  • Clinically Relevant, Cell-Based Assays – Leverage and implement any of the DiscoverX qualified or target-based bioassays to accelerate your biological candidate, whether it is a novel therapeutic or a biosimilar
  • Rigorously Tested Kinase Enzymes – Kinase enzymes utilized in KinaseProfiler™ services for screening millions of compounds over the past 30 years

 

Highlights of Kinase Product Solutions
Applications Benefits Product Portfolio Credibility
Screen for novel kinase inhibitors

Study kinase binding & pathways

Perform pharmacological profiling

Evaluate kinase receptor activation from therapeutic binding through downstream translocation

Measure RTK receptor dimerization, phosphorylation, internalization, & SH2-recruitment

Determine compound membrane penetration & kinase target binding

Analyze kinase activity & ADP accumulation		 Homogeneous assays with easy-to-use, rapid, no-wash protocols

Biologically relevant functional cell-based, MOA-reflective assays from discovery, through development, to QC lot release testing

Luminescent & fluorescent read-outs

Large recombinant kinase portfolio with broad coverage of human Kinome

Rigorous quality control & highly reproducible products (lot-to-lot)		 Stable cell lines

Ready-to-use eXpress & bioassay kits

Biologically relevant functional cell-based, MOA-reflective assays

Cell-based binding assays

Active, inactive, unactive, & mutant recombinant kinase enzymes
Kinase activity ADP accumulation kits

Custom product development		 Implemented in numerous biologics lot release programs globally

The original kinase company as part of Millipore / Upstate Biotechnologies

Assays, cell lines, enzymes, & assay platforms run by Eurofins Discovery KinaseProfiler & CRO screens daily

Helpful & experience customer support

Product Solution Guide and Target List:

Kinase and Phosphatase Product Solution Guide

 

Application Note:

Cellular Target Engagement Assays for Characterizing Novel Small Molecule Inhibitors of Oncogenic SHP2 Variants

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Kinase Recombinant Proteins, Cell Lines, and Ready-to-Assay eXpress & Bioassay Kits

  • Recombinant Kinase and Phosphatase Enzymes – Over 420 high-quality active, inactive, unactive, and mutant kinases, including many exclusive enzymes, including the PI3K and the PIKK group (ATM, ATR, mTOR, and DNA-PK)
  • Bioassay Kits – Qualified and target-based bioassays for evaluating RTK and cytokine receptor dimerization, SH2-recruitment, and IκB degradation, including CSF2, EGF, FGF, GH, IGF1, Insulin Receptor, Interleukin, ErbB2 (via HER2), PDGF, TrkA/B/C, and VEGF receptors including KDR
  • Kinase Receptor Assays – Functional and activity assays to analyze receptor dimerization, phosphorylation, internalization, and SH2-recruitment of RTKs
  • InCELL Target Engagement Assays – Compound-binding assays to confirm compound cell entry, measure intracellular kinase binding, screen and rank inhibitors, validate hits identified in biochemical assays, and measure cellular EC50 values all in the native cellular environment
  • Signaling Pathway Assays – NFκB/IκB kinase and PI3K/AKT signaling pathway assays to screen for inhibitors, monitor IκB degradation, and analyze receptor activation, phosphorylation, and downstream FOXO translocation
  • ADP Accumulation Assays – Antibody-free, homogeneous, and gain-of-signal activity-based assays for identifying and characterizing kinase phosphotransferase activity

Custom and Toolbox Products

  • Custom Capabilities – Custom cell lines and assays capabilities optimized to fit your requirements
  • Toolbox Products – Complete set of parental cell lines, expression and cloning vectors, kits, and retroparticles to build your own stable cell lines and cell-based assays.

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