
Product Description
MAPKAPK5 (MAPK-activated protein kinase 5), also known as MK5 or PRAK (p38-regulated/activated kinase), is a member of the serine/threonine protein kinase family (MAPKAPK subfamily) that plays a pivotal role in p38 MAPK and ERK3/4 signaling pathways, cell migration, cytoskeletal reorganization, and stress responses, as well as in cell cycle progression and gene expression regulation. MAPKAPK5 is activated by various stimuli including growth factors, oxidative stress, osmotic shock, and pro-inflammatory cytokines (e.g., TNFα), leading to downstream phosphorylation of substrates such as Hsp27, GADD153/CHOP, and HDAC4, thereby modulating actin dynamics, apoptosis, and transcriptional activity. Beyond its role in normal cellular homeostasis and stress adaptation, dysregulation of MAPKAPK5 signaling—through aberrant expression, hyperactivation, or genetic alterations—is closely associated with multiple cancers (including breast, lung, and colorectal cancer), chronic inflammation, and cardiovascular diseases (such as cardiac hypertrophy), making it a highly validated target for cancer therapy, anti-inflammatory drug discovery, and cardiovascular disease treatment.
Screeningbio’s MAPKAPK5 Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying MAPKAPK5 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: MAPKAPK5 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 MAPKAPK5 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_08364ec89c534bcea7bd0ed3c35bb477~mv2.png/v1/fill/w_49,h_46,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/cbf7de_08364ec89c534bcea7bd0ed3c35bb477~mv2.png)
