Cereblon Binding Assay Kit

Catalog #

79899

$600 *

Size: 96 reactions

Qty

Bulk/Custom

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*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.

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Synonyms

thalidomide

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Product Data Gallery

Product Info

Storage and Usage

Citations

Assay Kit Format

Fluorescence Polarization

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.

Storage/Stability

6 months when stored as recommended.

Instructions for Use

See assay protocol for detailed instructions.

Applications

Great for studying enzyme kinetics and screening small molecular inhibitors for drug discovery and HTS applications.

Shipping Temperature

-80°C

Warnings

*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.

Disclaimers and Limitations

BPS Bioscience assay kits are validated using the listed components according to our specific protocol. Any deviations to kit components or protocols, such as using different proteins, cell/tissue lysates, or buffers (including using the same component from other commercial sources) will void any warranties on the performance of the assay kit and is not recommended.

End-users should immediately report any issues to [email protected] upon receipt of the kit, such as missing components, damaged vials, no dry ice, etc.

Scientific Category

PROTAC

Regulatory Status

Research Use Only

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Cereblon Binding Assay Kit

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