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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: ERK1 (extracellular signal-regulated kinase 1) is also known as mitogen-activated protein kinase 3 (MAPK3), is a dual serine/threonine and tyrosine kinase. ERK (extracellular signal-regulated kinases), also known as classical MAPK (mitogen-activated protein kinases), are protein kinases involved in crucial intracellular signaling pathways, and regulate processes like mitoses, meiosis, and other functions. In the MAPK/ERK pathway Ras proteins are activated by several external molecules, including cytokines and viruses. These are followed by an activation cascade of c-Raf, MEK (mitogen-activated protein kinase kinase) and finally ERK. ERK1/2 in turn activates transcription factors. Disruption of the MAPK/ERK pathway at any point results in cancer. Inhibitors for Ras, Raf and MEK have been developed and result in rapid tumor reductions. However, resistance to treatment and relapse are quite frequent. This has led the field to focus on the development of ERK inhibitors, although these are difficult to design due to the high similarity to the CDK (cyclin-dependent kinase) pockets. Several ERK1/2 inhibitors are undergoing clinical trials aiming at treating advanced solid tumors, such as melanoma and adenocarcinoma, but further development and studies into ERK2 will open new therapeutic strategies in cancer oncology.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ ERK1 Kinase Assay Kit is designed to measure ERK1 (extracellular signal-regulated kinase 1) 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 recombinant ERK1, MBP, 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: P27361
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Busca R. et al., 2016 Front Cell Dev Biol 4:53.
Lavoie H., et al., 2020 Nature Reviews Molecular Cell Biology 21:607-623
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