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DYRK2 Kinase Assay

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Compound Test Services

CT-001

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Product Description


DYRK2 (Dual-specificity tyrosine phosphorylation-regulated kinase 2) is a member of the serine/threonine kinase family that plays a pivotal role in cell cycle regulation, apoptosis, and proteasomal degradation. DYRK2 is activated through autophosphorylation on tyrosine residues and subsequently phosphorylates downstream substrates such as p53, c-Myc, and components of the ubiquitin-proteasome system, thereby controlling cell survival, proliferation, and protein homeostasis. Beyond its essential physiological functions in tumor suppression and development, dysregulation of DYRK2 signaling—including loss of expression, impaired kinase activity, and altered substrate phosphorylation—is closely associated with various human cancers (such as breast cancer, colorectal cancer, and glioblastoma), as well as with metastatic progression and chemoresistance, making it a highly validated target for cancer therapy and drug discovery.


Screeningbio’s DYRK2 Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying DNA-PK kinase activity and evaluating the potency of tyrosine kinase inhibitors (TKIs).


This kit utilizes the ADP-Glo Kinase Assay platform, a luminescent technology that measures the amount of ADP produced during the kinase reaction.

The assay is performed in two distinct steps:

  1. Kinase Reaction: DYRK2 catalyzes the transfer of a phosphate group from ATP to a specific substrate, resulting in the production of phosphorylated substrate and ADP.

  2. ADP-Glo™ Reagent Addition: After the kinase reaction, the ADP-Glo™ Reagent is added to terminate the reaction and deplete any remaining unreacted ATP.

  3. Kinase Detection: The Kinase Detection Reagent is added to simultaneously convert the produced ADP back into ATP, which is then used by luciferase to generate a luminescent signal.

The light intensity produced is directly proportional to the ADP concentration and, consequently, to the enzymatic activity of the DYRK2 kinase.



Data

TKs Kinase Inhibition Assay. Staurosporine was titrated using established assay protocol. Non-linear regression was used to plot RLU signal vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.
TKs Kinase Inhibition Assay. Staurosporine was titrated using established assay protocol. Non-linear regression was used to plot RLU signal vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.


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