
Product Description
KDR (Kinase insert domain receptor), also known as VEGFR2 (Vascular endothelial growth factor receptor 2) or CD309, is a member of the receptor tyrosine kinase (RTK) family that plays a pivotal role in angiogenesis, vasculogenesis, vascular permeability, and endothelial cell survival, proliferation, and migration. KDR is activated by various stimuli including VEGF-A, VEGF-C, and VEGF-D, leading to downstream activation of the PLCγ/PKC/Raf/MEK/MAPK, PI3K/AKT, and Src/FAK pathways, thereby regulating endothelial cell function and blood vessel formation. Beyond its role in normal vascular development and homeostasis, dysregulation of KDR signaling—through overexpression, hyperactivation, or gain-of-function mutations—is closely associated with tumor angiogenesis, metastasis, neovascular eye diseases (including age-related macular degeneration and diabetic retinopathy), and cardiovascular disorders, making it a highly validated target for anti-angiogenic cancer therapy (e.g., tyrosine kinase inhibitors and monoclonal antibodies) and ophthalmic drug discovery.
Screeningbio’s KDR Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying KDR 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:
Kinase Reaction: KDR catalyzes the transfer of a phosphate group from ATP to a specific substrate, resulting in the production of phosphorylated substrate and ADP.
ADP-Glo™ Reagent Addition: After the kinase reaction, the ADP-Glo™ Reagent is added to terminate the reaction and deplete any remaining unreacted ATP.
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 KDR 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.](https://static.wixstatic.com/media/cbf7de_d64524cb87c24c25a02a125a01c1f2bf~mv2.png/v1/fill/w_49,h_46,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/cbf7de_d64524cb87c24c25a02a125a01c1f2bf~mv2.png)
