Product Description

Tyrosine kinases are a large family of enzymes that catalyze the transfer of a phosphate group from ATP to the hydroxyl group of tyrosine residues on target proteins. This phosphorylation serves as a critical regulatory mechanism in numerous cellular processes, including growth, differentiation, metabolism, and apoptosis. Tyrosine kinases are broadly classified into receptor tyrosine kinases (RTKs), such as EGFR, VEGFR, and FGFR, which span the cell membrane and respond to extracellular ligands, and non-receptor tyrosine kinases (NRTKs), such as Src, JAK, and Abl, which function within the cytoplasm. Dysregulation or mutation of tyrosine kinases can lead to aberrant signaling and is a hallmark of many cancers and inflammatory diseases. Consequently, tyrosine kinase inhibitors (TKIs) have become a major class of targeted therapies, effectively blocking overactive kinase signaling in conditions such as chronic myeloid leukemia and non-small cell lung cancer.

Screeningbio’s TR-FRET tyrosine kinase assay kit is designed to measure the relative activity levels of kinases. The kit assay utilizes a biotin-labeled, optimized peptide substrate that binds to TR-FRET HX–conjugated streptavidin. When combined with a phospho-tyrosine–specific antibody conjugated to TR-FRET Solar Eu, the degree of substrate phosphorylation can be quantitatively measured via TR-FRET signal intensity, which is directly proportional to kinase activity.

This assay kit adopts the TR-FRET (time-resolved fluorescence resonance energy transfer)–based immunoassay method, which is simple, fast, highly specific, sensitive, and reproducible.

This homogeneous, no-wash immunoassay offers exceptional specificity, sensitivity, and reproducibility, providing a robust platform for TKs inhibitor screening, kinase profiling, and drug discovery research.

During the assay, kinase catalyzes phosphorylation of the substrate in the presence of ATP. The reaction is then terminated with EDTA, followed by antibody binding to the phosphorylated substrate. Energy transfer between the donor and acceptor fluorophores generates a TR-FRET signal upon excitation, with signal intensity directly proportional to the phosphorylation level.