Cereblon Binding Assay Kit

Catalog #
79899
$600 *
Size: 96 reactions
Qty
*US Pricing only. For international pricing, please contact your local distributor.
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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 a positive 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. The FP signal is measured using a fluorescent microplate reader capable of measuring fluorescence polarization.

Need us to run inhibitor screens or profile your compounds against Cereblon Binding? Check out our Ubiquitination Screening Services.

Synonyms
thalidomide
Product Info
Storage and Usage
Citations
Assay Kit Format
Fluorescence Polarization
Species
Human
Supplied As
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.
Materials Required But Not Supplied

Adjustable micropipettor
Sterile tips

Format
Catalog # Component Amount Storage
100255 FLAG-CRBN 60 µg -80°C Avoid
freeze/
thaw
cycles
  Cy5-labeled Thalidomide*, 10 μM 15 µl -80°C
79972 CRBN Assay buffer (FP) 10 ml -80°C
  Pomalidomide, 50 mM 15 µl -20°C
79685 Black, low binding, microtiter plate 1 Room
Temp
 

 

UniProt #
Q96SW2
References

1. Lopez-Girona A , et al., Leukemia 2012; 26: 2326-35.
2. Fischer ES, et al., Nature 2014; 3512 (7512): 49-53.