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Application: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: SRC (proto-oncogene tyrosine kinase SRC), also known as c-SRC, belongs to the non-receptor tyrosine kinase (SFK) protein family. It is involved in embryonic development, cell growth, adhesion, migration, differentiation, and apoptosis. It is present in an inactive conformation until activated by adhesion receptors, receptor tyrosine kinases such as EGFR (epidermal growth factor receptor) and PDGFR (platelet-derived growth factor receptor), G-protein coupled receptors, and cytokine receptors. Phosphorylation at Tyr527 by CSK/MATK (C-terminal Src kinase) or ChK (CSK homolog kinase) and dephosphorylation at Tyr416 by phosphatases leads to its activation. Once active it phosphorylates its substrates, which include PI3Ks (phosphoinositide 3-kinases), cytoskeleton proteins, channel proteins and metabolic enzymes, participating in multiple pathways. It is a proto-oncogene, with overexpression and overactivation resulting from mutations, increased expressions of its activators or decrease of its inactivators, being found in glioblastoma (GBM), lung, liver, breast, bladder cancer, and others. Several inhibitors of this protein have been studied, and Dasatinib has been approved for treatment of hematologic tumors. However, the possible side effects and development of drug resistance have been a concern. The development of new therapeutic strategies towards this protein will bring advances into oncology.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ SRC Kinase Assay Kit is designed to measure SRC (proto-oncogene tyrosine kinase SRC) 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 SRC, 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: P12931
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: PelazS.andTaberneroA.,2022Oncogene41:4917-4928.