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c-MER Kinase Assay

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Compound Test Services

CT-001

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Product Description


c-MER, also known as MERTK (MER proto-oncogene tyrosine kinase), is a member of the receptor tyrosine kinase (RTK) family belonging to the TAM (Tyro3-AXL-MER) subfamily, which plays a pivotal role in phagocytosis, immune regulation, cell survival, and tissue homeostasis. c-MER binds with high affinity to its ligands, growth arrest-specific protein 6 (Gas6) and Protein S, leading to activation of downstream signaling pathways such as PI3K/AKT, MAPK, and STATs. Beyond its essential physiological functions in efferocytosis (clearance of apoptotic cells) and immune suppression, dysregulation of c-MER signaling—including overexpression, constitutive activation, and aberrant expression—is closely associated with various cancers (such as acute myeloid leukemia, glioblastoma, melanoma, and non-small cell lung cancer), contributing to tumor progression, metastasis, immune evasion, and resistance to chemotherapy and immunotherapy. These features have established c-MER as a highly validated target for cancer therapy and drug discovery.


Screeningbio’s c-MER Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying c-MER 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: c-MER 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 c-MER 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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