Kinase Selectivity Profiling Systems

Description

The Kinase Selectivity Profiling Systems are easy-to-use kits for performing kinase selectivity profiling that rely on the ADP-Glo™ Kinase Assay technology (Figure 1). Each system includes kinase and substrate pairs organized in an easy-to-use 8-tube strip format optimized for fast and simple kinase profiling reactions (see Figures and Tables tab for complete listing of enzymes and substrates).

Kinase Selectivity Profiling Systems offer kinases grouped either in single kinase family strips or as a general panel of kinases representative of the human kinome for a broad kinase profile. Each profiling system contains the reagents needed to complete a profile for a compound, including kinase reaction buffer, eight kinases in each multiwell strip and eight corresponding substrates and cofactors in another multiwell strip (Figure 2). The General Panel contains 24 kinases arranged in three 8-well strips.

If you do not see a kinase selectivity profiling system that meets your experimental needs, you can design your own custom system using the custom kinase selectivity profiling system tool.

Features – Benefits

• Fast Turnaround Time: Lead compounds can be profiled in-house in a matter of hours versus days when compounds are sent out.
• Flexible Kinase Inhibitor Profiling: Each system has enough material to profile up to twenty compounds at a single dose or create a dose-response for two compounds against the eight kinases at once.
• Fast and Simple Reaction Assembly: Two quick dilutions provide working stocks of kinases and substrate/cofactor solutions.
• Optimized Kinase Activity for Inhibitor Profiling: All kinases have been optimized to provide 10–30% ADP production when assayed at 10µM ATP.
• Formatted Strips Provide Access to Eight Kinases at One Time: Kinases from singular kinase families are grouped together for a more relevant selectivity profile.
• Accurate: Accurately measure ADP levels at a wide range of starting ATP concentrations; activity measured truly reflects kinase activity and produces accurate IC₅₀ values comparable to radioactivity-based assays.
• Stable Luminescent Signal: Perform batch plate processing without need for strictly timed incubations; flexible.

Applications

• Selectivity screening of library compounds for effects on target kinases.
• Profile hits and leads for their potency against families of related kinases.