Bisubstrate fluorescent probes for protein kinase CK2

摘要

This invention relates to fluorescent probes for screening and characterization of compounds binding to protein kinase CK2, measurement of concentration of the catalytically active form of CK2 and imaging of CK2 activity in cells and tissues. The CK2-selective probe of the present invention interacts with binding sites of both substrates of the catalytic subunit of CK2 and therefore can be used for characterization of all inhibitors binding to the active site of CK2 in the binding/displacement assay. The high affinity of the probe affords the detection of the enzyme at low concentration and characterization of inhibitors in a wide affinity range.