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ARC-Photo Fluorescence Polarization Kinase Binding Assay Kit
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Screening and characterization of inhibitors of protein kinases (PK) is usually performed in the form of kinetic studies where the retarding effect of the compound on the rate of kinase-catalyzed phosphorylation reaction is assigned. Alternatively, kinase inhibitors may be identified by direct or indirect measurement of binding of the compound to the kinase.
The kit ARC-Photo is applicable in competition displacement assays for identification and characterization of inhibitors of many protein kinases and determination of the active (binding) concentration of a protein kinase. The fluorescent probe ARC-Photo has very high affinity towards several kinases (e.g., Kd < 1 nM for cAMP-dependent protein kinase, PKA). The bisubstrate-analog character of the probe (the inhibitor ARC simultaneously binds to both pockets of PK) enables the characterization of inhibitors (and substrates) targeted to ATP binding site and/or substrate protein/peptide binding domain of the kinase.
As tested in a panel of 52 protein kinases ARC-type compounds are good inhibitors of basophilic PK (neighborhood of phosphorylation sites of substrates is rich in arginine and/or lysine residues). Thus ARC-Photo is a potential fluorescent probe for many kinases with such qualities (e.g., majority of PK of the AGC group are basophilic).
Key features of the kit:
ARC-Photo is a fluorescent probe with excellent characteristics:
High chemical and photo-stability, soluble in water;
Long wave-length fluorescence (540 nm excitation and 590 nm emission with
20 nm bandpass filters);
Large signal window (> 130 mA) ensures high Z' factors of > 0.7.
Compare ARC-Photo with other available products on the market!
Mechanism of ARC-Photo