Product Description
KHS1 (Kinase homologous to SPS1/STE20), also known as MAP4K5 (mitogen-activated protein kinase kinase kinase kinase 5) or GCKR (germinal center kinase-related enzyme), is a member of the serine/threonine protein kinase family (STE20/GCK subfamily) that plays a pivotal role in stress-activated protein kinase (SAPK/JNK) signaling, immune regulation, and Wnt-mediated B‑cell functions, as well as in cell proliferation, apoptosis, and cytoskeletal organization. KHS1 is activated by various stimuli including TNFα, TRAF2, CD40 engagement, UV irradiation, and oxidative stress, leading to downstream activation of the JNK and p38 MAPK pathways, as well as modulation of SAPK signaling, thereby influencing stress responses and cell fate decisions. Beyond its role in normal immune cell signaling and tissue homeostasis, dysregulation of KHS1 signaling—through loss-of-function mutations, aberrant expression, or altered kinase activity—is closely associated with multiple cancers (including colorectal, ovarian, liver, skin, and endometrial cancers), chronic inflammatory diseases (such as inflammatory bowel disease), and cardiovascular disorders, making it a highly validated target for cancer therapy (particularly in ovarian and liver cancers) and drug discovery.
Screeningbio’s KHS1 Kinase Assay Kit provides a robust, sensitive, and high-throughput platform for quantifying KHS1 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: KHS1 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 KHS1 kinase.
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