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.
Product Highlights
- 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
- 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
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 |
Access Products by Target
Comprehensive Offering of Cellular Assays and Recombinant Enzymes for Drug Discovery Screening and Lead Optimization
Read MoreComprehensive Eurofins DiscoverX product list to enable your drug discovery and development programs focused on checkpoint receptors, cytokine receptors/interleukins, cytotoxicity,…
Read MoreIt is well established that ligand binding can protect proteins from thermal denaturation in a cellular milieu; however, the broad…
Read MoreBoth multi- and single-pass membrane receptors constitutively exhibit complicated and dynamic membrane receptor trafficking as well as internalization induced by…
Read MoreCell-based bioassays often pose a hurdle during a rapidly moving biologics development program. High standards for assay accuracy, precision, reproducibility…
Read MoreCell-based bioassays often pose a hurdle during a rapidly moving biologics development program. High standards for assay accuracy, precision, reproducibility…
Read MoreOne of the major bottlenecks in the development of biosimilars is the need for good bioassays to create potency, stability…
Read MoreDiscoveRx’s PathHunter® platform is a simple, cell-based, chemiluminescent assay format that allows for screening large numbers of small molecules or…
Read MoreAssays that directly detect compound binding inside cells can be of great utility in translating in vitro data to more…
Read MoreDrug efficacy and cellular target engagement studies have traditionally been monitored by evaluation of downstream cellular responses, such as detection…
Read MoreDiscoveRx has developed a unique assay technology based on an enzyme-coupled detection system that measures ADP accumulation which has been…
Read MoreAssays that directly detect compound binding inside cells can be of great utility in translating in vitro data to more…
Read MoreThere are numerous assays available to measure the activity of enzymes involved in the transfer of a phosphate from ATP…
Read MoreKinase targets have been extensively studied in biochemical assays using purified protein fragments for the kinase and the substrate. However,…
Read MoreKinase targets have been extensively studied in biochemical assays using purified protein fragments for the kinase and the substrate. However,…
Read MoreKinase targets have been extensively studied in biochemical assays using purified protein fragments for the kinase and the substrate. However,…
Read MoreThe PathHunter™ technology from DiscoveRx is an adaptation of Enzyme Fragment Complementation (EFC) that provides a novel, generic cell-based assay…
Read MoreKinase therapeutics includes both monoclonal antibodies (mAbs) and small-molecule inhibitors. DiscoveRx’s PathHunter® protein: protein interaction system uses well-established Enzyme Fragment…
Read MoreThe webinar focuses on utilizing an InCELL Pulse to characterize small-molecule cellular target engagement. As an example, a case study…
Watch NowProtein kinases are critical to many cellular pathways and play a role in several therapeutic areas such as oncology, inflammation,…
Watch NowHere we will describe InCELL Pulse™, which uses DiscoverX’s Enzyme Fragment Complementation (EFC) technology to overcome these limitations of current…
Watch NowKinase inhibitors often potently inhibit several off-target kinases in biochemical assays. Unfortunately, the relevance of these off-target interactions in a…
Watch NowIt is well established that ligand binding can protect proteins from thermal denaturation in a cellular milieu; however, the broad…
Watch NowHistone modifications are essential in eukaryotic gene expression and regulation, and are driven by histone writer, eraser, and reader proteins.…
Read MoreSHP2 (Src-homology 2 domain-containing phosphatase 2) is a protein tyrosine phosphatase encoded by the human PTPN11 gene.SHP2 is a key…
Read MoreLearn how InCELL cell-based binding assays can be used to detect compound cell entry and engagement to specific targets including…
Watch NowLearn about PathHunter Internalization assays developed to measure translocation of both single-pass and multi-pass receptors (like RTKs, checkpoint receptors and…
Watch NowLearn how functional cell-based assays support COVID-19 drug discovery programs, particularly in managing proinflammatory cytokines associated with high mortality rate…
Watch NowLearn about Eurofins DiscoverX cell line engineering, assay development, and recombinant enzyme production custom capabilities. Find out more about cell…
Watch NowInformation on compound-target engagement obtained from traditional in vitro binding assays differs greatly from that in a physiologically relevant model…
Read MoreWhether you’re looking to screen a library of drug candidates for binding to a particular target protein, checking drug cell…
Read MoreCell-based assays are useful for understanding cellular pathways; characterizing targets and their function; identifying, screening, and optimizing ligands or drugs…
Read MoreThe development of new medicines for treating diseases and new chemical probes for elucidating biological function continues to rely on…
Read MoreThe non-receptor protein tyrosine phosphatase (PTP) SHP2 is encoded by the proto-oncogene PTPN11 and is a ubiquitously expressed key regulator…
Read MoreFYVE-type zinc finger-containing phosphoinositide kinase (PIKfyve) catalyzes the formation of phosphatidylinositol 3,5-bisphosphate (PI(3,5)P2) from phosphatidylinositol 3-phosphate (PI(3)P).
Read MoreIn this study, we describe the evaluation of a cell-based protein stability assay using β-galactosidase fragment complementation technology performed in…
Read MoreOwing to their central role in regulating cell signaling pathways, the phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) are attractive therapeutic targets in…
Read MoreA series of substituted indoles were examined as selective inhibitors of tropomyosin-related kinase receptor A (TrkA), a therapeutic target for…
Read MorePhosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) are emerging as attractive therapeutic targets in diseases, such as cancer, immunological disorders, and neurodegeneration, owing…
Read MoreBrain-derived neurotrophic factor (BDNF) and its receptor, tropomyosin-related kinase B (TrkB), have emerged as key regulators of brain plasticity and…
Read MoreSystemic therapy of advanced hepatocellular carcinoma (HCC) with the small molecule multi-kinase inhibitor sorafenib is associated with large inter-individual pharmacokinetic…
Read MoreCurrent therapies for chronic pain can have insufficient efficacy and lead to side effects, necessitating research of novel targets against…
Read MoreStrong genetic data link the Tyrosine kinase receptor B (TrkB) and its major endogenous ligand brain-derived neurotrophic factor (BDNF) to…
Read MoreFunctional Cell-Based Assays, Cell Lines, & Proteins for Cancer Research Improved or novel small molecule or biologic therapeutics for cancer…
Read MoreRobust Cell-Based Assays to Identify Therapeutic Hits Rapidly
Read MoreProducts & Custom Development Capabilities.
Read More
Antibody-free, homogeneous assays to monitor ATP depletion & ADP accumulation in cells for kinase profiling applications
Read More
Functional & activity assays to analyze receptor dimerization, phosphorylation, internalization, & SH2-recruitment of RTKs & CTK/cytokine receptors
Read More
Screening cell-based assays for analyzing the movement of proteins to multiple membrane compartments within the cell
Read More
Interrogate a variety of popular target-specific pathways with cell-based assays
Read More
Cell-based assays to confirm compound cell entry, protein target binding, screen & rank inhibitors, & measure cellular potencies
Read More
Complete set of parental cell lines, vectors, kits, & retroparticles to build your own stable cell lines & cell-based assays
Read More
Custom cell lines, kits, assays, & protein development capabilities optimized to fit your requirements
Read More