
Product Description
c-Kit, also known as CD117 or KIT, is a member of the receptor tyrosine kinase (RTK) family (type III subfamily) that plays a pivotal role in hematopoiesis, melanogenesis, gametogenesis, and mast cell development. c-Kit binds with high affinity to its ligand, stem cell factor (SCF), leading to receptor dimerization and activation of downstream signaling pathways such as PI3K/AKT, MAPK, and Src family kinases. Beyond its essential physiological functions, dysregulation of c-Kit signaling—including activating mutations, gene amplification, and overexpression—is closely associated with various human cancers such as gastrointestinal stromal tumors (GISTs), acute myeloid leukemia, mastocytosis, and melanoma, as well as with systemic mastocytosis and other proliferative disorders. These features have established c-Kit as a highly validated target for cancer therapy and drug discovery, exemplified by the clinical success of tyrosine kinase inhibitors such as imatinib.
Screeningbio’s c-Kit Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying c-Kit 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: c-Kit 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 c-Kit 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_70e2caa2fc164de187a7f59be031cf2d~mv2.png/v1/fill/w_49,h_45,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/cbf7de_70e2caa2fc164de187a7f59be031cf2d~mv2.png)
