Cereblon Binding Assay Kit
BPS-79899 96 reactions
Data Sheet: 
Applications
Great for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications.
Shipment
-80°C (dry ice)
Literature References
1. Lopez-Girona A , et al., Leukemia 2012; 26: 2326-35.
2. Fischer ES, et al., Nature 2014; 3512 (7512): 49-53.
2. Fischer ES, et al., Nature 2014; 3512 (7512): 49-53.
Description
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. - Great for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications. - *Thalidomide is known to cause severe birth defects in humans. It is very important to use all appropriate precautions when handling this compound, especially by pregnant women.
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. - Great for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications. - *Thalidomide is known to cause severe birth defects in humans. It is very important to use all appropriate precautions when handling this compound, especially by pregnant women.
ESCLUSIVAMENTE PER USO DI RICERCA (RUO) e non per uso terapeutico o diagnostico su uomini o animali. Il prodotto NON è un Dispositivo Medico o un Diagnostico in Vitro.
PRODUCT FOR RESEARCH USE ONLY (RUO) and not for therapeutic or diagnostic use on humans or animals. The product is NOT a Medical Device or an In-Vitro Diagnostic (IVD).
