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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: HER4 (human epidermal growth factor receptor 4), also known as ErbB4 or receptor-tyrosine kinase 4, is a receptor tyrosine kinase protein of the EGFR family. It is required for the development of the heart, nervous system, and mammary gland, and can also be found in the postsynaptic side of neuromuscular junctions and epidermis. HER4 is activated by neuroregulin 2-4, betacellulin and heparin binding EGF-like growth factor (HB-EGF) and is involved in mitogenesis and cell differentiation. HER4 undergoes a conformational change upon ligand binding and forms homodimers or heterodimers with other HER proteins to activate the MAPK (mitogen-activated protein kinases) and PI3K (phosphoinositide 3-kinase)/AKT pathways. Mutations in this protein can result in cancer but have also been linked to ALS (amyotrophic lateral sclerosis) type 19 and schizophrenia. The role of this protein as oncogene or suppressor is still not fully determined, potentially being dependent on the cancer type. Several HER4 inhibitors have been developed and are undergoing clinical trials. Afatinib, a pan-HER inhibitor, has been approved for the treatment of NSCLC (non-small cell lung cancer), but may cause acute liver injury and death. The development of highly specific inhibitors for HER4 may prove beneficial in oncology.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ HER4 Kinase Assay Kit is designed to measure HER4 (human epidermal growth factor receptor 4) tyrosine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified HER4 (amino acids 708-993), kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed
Uniprot: Q15303
Warnings: Avoid freeze/thaw cycle
Biosafety Level: Not applicable (BSL-1)
References: El-Gamal M., et al., 2021. Molecules 26(23):7376.
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