
Product Description
MELK (Maternal embryonic leucine zipper kinase), also known as MPK38 or p38K, is a member of the serine/threonine protein kinase family (AMPK-related kinase subfamily) that plays a pivotal role in cell cycle progression, stem cell self-renewal, apoptosis regulation, and embryonic development, as well as in spliceosome assembly and DNA damage response. MELK is activated by various stimuli including cell cycle signals, phosphorylation by CDK1/cyclin B, and stress conditions, leading to downstream phosphorylation of substrates such as CDC25B, Bcl-xL, and Geminin, thereby promoting G2/M transition, inhibiting apoptosis, and supporting cancer cell survival. Beyond its role in normal embryogenesis and tissue homeostasis, dysregulation of MELK signaling—through overexpression or aberrant kinase activity—is closely associated with multiple cancers (including glioblastoma, breast cancer, prostate cancer, and colorectal cancer), where it contributes to tumor proliferation, chemoresistance, and poor prognosis, making it a highly validated target for cancer therapy and drug discovery.
Screeningbio’s MELK Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying MELK 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: MELK 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 MELK 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_cf78e62f5e804a2e91b8961eb74d3cf4~mv2.png/v1/fill/w_49,h_46,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/cbf7de_cf78e62f5e804a2e91b8961eb74d3cf4~mv2.png)
