PhosphoSens DYRK1A Protein Kinase Assays, Substrates & Recombinant Enzymes

Continuous, real-time assays that directly quantify DYRK1A catalytic activity — generating a full progress curve in every well for IC₅₀, mechanism, and selectivity studies.

  • Real-time kinetic or TRF endpoint formats
  • Optimized substrates and assay-ready kits
  • Compatible with physiological ATP and cofactors

Designed for: drug discovery, lead optimization, and mechanistic kinase research teams

 

PhosphoSens DYRK1A kinase assay kit — continuous real-time fluorescence

About DYRK1A

DYRK1A (Dual Specificity Tyrosine Phosphorylation-Regulated Kinase 1A) belongs to the DYRK subfamily of the CMGC kinase group, characterized by their ability to phosphorylate both tyrosine and serine/threonine residues. DYRK1A undergoes autophosphorylation on a conserved tyrosine residue (Tyr321) within its activation loop during translation, a unique cis-autophosphorylation mechanism that locks the kinase in a constitutively active conformation. Key substrates include tau (phosphorylation at Thr212), NFAT transcription factors, cyclin D1, and the splicing factor SRSF6, placing DYRK1A at the crossroads of neuronal development, cell cycle regulation, and alternative splicing. The kinase is encoded on chromosome 21 and is overexpressed in Down syndrome (trisomy 21), contributing to intellectual disability and early-onset Alzheimer's disease pathology. DYRK1A haploinsufficiency causes a distinct intellectual disability syndrome, underscoring its dosage sensitivity. These roles make DYRK1A a compelling therapeutic target in neurodegenerative disease, Down syndrome cognitive deficits, and certain cancers including glioblastoma and leukemia.

Why PhosphoSens for DYRK1A?

DYRK1A drug discovery faces several assay challenges: the kinase phosphorylates both Tyr and Ser/Thr residues, complicating antibody-based detection; its constitutive activity requires careful enzyme titration to avoid substrate depletion artifacts in endpoint formats. ADP-Glo and HTRF measure single time-point endpoints, masking nonlinear kinetics caused by substrate inhibition or slow-binding inhibitors common among DYRK1A chemotypes such as harmine-class alkaloids. Radiometric assays require hazardous isotopes and lack temporal resolution. PhosphoSens continuous fluorescent assays monitor phosphorylation in real time using CSox-based peptide substrates, generating complete progress curves at physiological ATP concentrations. This enables accurate Km(ATP) determination critical for selectivity profiling, captures covalent inhibitor kinact/KI parameters without specialized secondary assays, and eliminates inner-filter artifacts. Real-time kinetics also reveal mechanistic nuances of DYRK1A inhibition mode, accelerating structure-activity relationship campaigns.

Key Pathways: NFAT/Calcineurin signaling Tau/Alzheimer neurodegeneration Hedgehog/Gli signaling Cell cycle G1-S regulation

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Real-Time DYRK1A Activity Assays

Continuous, real-time fluorescent assays optimized for quantitative DYRK1A activity measurements, IC50 determination, and mechanistic studies.

Assay Format: Continuous kinetic fluorescence (real-time)

PhosphoSens-Kinetic assays directly quantify enzyme activity by continuously monitoring substrate phosphorylation or dephosphorylation in real time, generating a full progress curve in every well.

Learn more about PhosphoSens-Kinetic →

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Kits

PhosphoSens-Kinetic Kinase Activity Kit - AQT0260

Ready-to-use assay kits containing substrate and all essential reagents.

Kit Contents
  • Optimized PhosphoSens® substrate (AQT0260)
  • ATP, DTT, EGTA, Reaction Buffer & Dilution Buffer

Automatically save 10% when bundling 10ug recombinant enzyme with your 1,000 assay kit. View enzymes

Price: $425

Substrate

PhosphoSens Kinase Substrate AQT0260

Bulk PhosphoSens® substrate for assay development and high-throughput workflows.

Specifications

Automatically save 10% when bundling Reagent Packs with your substrate. View Reagent Packs

Price: $2795

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No PhosphoSens-Red format is currently available for DYRK1A.

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Active Recombinant Enzymes for DYRK1A

Wild-type and mutant forms of DYRK1A for assay development, kinase profiling, and mechanistic studies. Enzymes are supplied active and optimized for PhosphoSens® substrates.

DYRK1A, Active Full Length

Rat • E. coli

Technical Specifications
  • Catalog: AQT-D09-10G
  • Mutation: Full Length
  • Species: Rat
  • Expression System: E. coli
  • Storage Buffer: Supplied as sterile 50 mM Tris-HCl, pH 7.5, 50-300mM NaCl, 10mM glutathione, 0.1mM EDTA, 0.25-1.0mM DTT, 0-0.1mM PMSF, 10-25% glycerol
  • Molecular Weight: ~100 kDa
  • Purity/Activity: For specific information on a given lot, see related technical data sheet.
  • Storage Conditions: Store product at -70°C. For optimal storage, aliquot target into smaller quantities after centrifugation and store at recommended temperature. For most favorable performance, avoid repeated handling and multiple freeze/thaw cycles.
Available Sizes:

Price: $$378.00

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Frequently Asked Questions: DYRK1A Assays

What peptide substrate does AssayQuant use for DYRK1A PhosphoSens assays?

AssayQuant offers optimized CSox-based peptide substrates derived from validated DYRK1A phosphorylation consensus sequences, designed to report phosphorylation via real-time fluorescence. The substrates are validated for linearity, Km determination, and compatibility with compound libraries, ensuring robust signal windows across a range of enzyme concentrations.

Can PhosphoSens DYRK1A assays distinguish inhibitor binding modes such as ATP-competitive versus substrate-competitive?

Yes. Because PhosphoSens generates continuous progress curves at variable ATP and substrate concentrations, full Michaelis-Menten analysis can be performed to resolve competitive, uncompetitive, and mixed inhibition modes. This mechanistic detail is unavailable from single-timepoint ADP-Glo or HTRF readouts and is critical for understanding selectivity among DYRK family members.

Is the DYRK1A assay compatible with physiological ATP concentrations for selectivity profiling?

PhosphoSens assays are routinely run at or near physiological ATP concentrations (1 mM), unlike radiometric or luminescence assays that artificially lower ATP to maximize signal. Running at physiological ATP provides IC50 values that better reflect cellular potency and enables accurate selectivity comparisons across DYRK1A, DYRK1B, CLK1, and related kinases.

Data & Resources

Explore data and documents to support your kinase and phosphatase experiments. Download sample data, protocols and other resources to see how our assays perform and to help you get started in your own lab. All validation data generated using PhosphoSens® assays under recommended conditions.

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