
Product Description
InsR (Insulin Receptor), also known as CD220 or INSR, is a member of the receptor tyrosine kinase (RTK) family that plays a pivotal role in glucose homeostasis, metabolic regulation, cell growth, and survival. InsR is activated by insulin binding, leading to autophosphorylation and downstream activation of the PI3K/AKT and RAS/RAF/MAPK signaling pathways, thereby promoting glucose uptake, glycogen synthesis, and lipid metabolism. Beyond its role in normal metabolic control, dysregulation of InsR signaling—through loss-of-function mutations, impaired kinase activity, or reduced expression—is closely associated with diabetes mellitus, insulin resistance, metabolic syndrome, and certain cancers (including breast and colorectal cancer), where it contributes to hyperglycemia, dyslipidemia, and therapy resistance, making it a highly validated target for metabolic disease therapy and cancer drug discovery.
Screeningbio’s InsR Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying InsR 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: InsR 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 InsR 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_f706001821eb443693ad929f7f5965d1~mv2.png/v1/fill/w_49,h_46,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/cbf7de_f706001821eb443693ad929f7f5965d1~mv2.png)
