Cereblon Binding Assay Kit

The Cereblon Binding Assay Kit (FP) is designed for testing and profiling of Cereblon (CRBN) inhibitors using Fluorescence Polarization. The assay is a competitive binding assay, based on the binding of fluorescently-labeled Thalidomide, a CRBN binder, to purified recombinant CRBN. CRBN is the substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins. CRBN is a direct protein target for the immunomodulatory and antiproliferative activities of thalidomide analogues such as lenalidomide and pomalidomide. The Cereblon Binding Assay Kit (FP) comes in a convenient 96-well format, with enough purified CRBN, Cy5-labeled Thalidomide, and assay buffer for 100 enzyme reactions. In addition, the kit includes the CRBN inhibitor Pomalidomide for use as an inhibitor control.
The key to the CRBN Assay Kit is the fluorescently-labeled Thalidomide. Using this kit, only one simple step on a microtiter plate is required for CRBN reactions. The Cy5-labeled Thalidomide is incubated with a sample containing CRBN to produce a change in fluorescent polarization that can be measured using a fluorescence reader.

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