PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding

Catalog #

79770

$995 *

Size: 384 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 PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding is designed for testing and profiling of PROTACs® directed against BET Bromodomain family and Cereblon complex. Cereblon (CRBN) is a Substrate recognition component of a DCX (DDB1-CUL44-Rbx1) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins.

With this kit, only three simple steps on a microtiter plate are required for PROTAC® activity detection. First, a sample containing PROTAC® is incubated with CRBN and BRD3(BD2), one of the BET bromodomains. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.

Assay Principle

Need us to run inhibitor screens or profile your compounds against PROTAC® Optimization for BET Bromodomain-Cereblon Binding? Check out our Bromodomain Screening Services or PROTACs ® & Protein Degradation Services.

This product has been cited 5 times.

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Synonyms

CRBN, Protein X 0001, MRT2A MRT2, Bromodomain containing 3, BRD3, RING3L

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Product Data Gallery

Product Info

Storage and Usage

Citations5

Assay Kit Format

AlphaLISA®

Supplied As

The PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding comes in a convenient AlphaLISA® format, with enough dBET1 PROTAC®, Immuno Buffer 1, purified BRD3(BD2) and CRBN for 384 reactions. (+)JQ1 is included as a control inhibitor of PROTAC® binding to BRD3(BD2).

Materials Required But Not Supplied

AlphaLISA anti-FLAG acceptor beads, 5 mg/ml (PerkinElmer #AL112C)
Alpha Glutathione donor beads, 5 mg/ml (PerkinElmer #6765300)
Optiplate 384 (PerkinElmer #6007290)
AlphaScreen microplate reader
Adjustable micropipettor and sterile tips

Format

Catalog #	Component	Amount	Storage
100329	Cereblon/DDB1/Cul4A/ Rbx1 Complex	30 µg	-80°C	Avoid freeze/ thaw cycles
31033	BRD3(BD2), GST-tag	5 µg	-80°C
	dBET1 (1 mM)	10 µl	-80°C
79311	3x Immuno Buffer 1	4 ml	-20°C
27403	(+)-JQ1 (10 mM)	10 µl	-20°C

*Concentration of Cereblon and BRD3 will be indicated on the tube containing protein

References

Winter, G.E., Paulk, J., Roberts, J.M., et al. Science 2015; 348(6241):1376-81.

Storage/Stability

At least six months from date of receipt when stored as directed.

Instructions for Use

See assay protocol for detailed instructions.

Applications

Great for the characterization of PROTACs® targeting the BET family of bromodomains, design of novel molecules targeting CRBN, and comparison of the activities of different PROTACs®.

Shipping Temperature

-80°C

Contraindications

Green and blue dyes that absorb light in the AlphaScreen signal emission range (520-620 nm), such as Trypan Blue. Avoid the use of the potent singlet oxygen quenchers such as sodium azide (NaN₃) or metal ions (Fe²⁺, Fe³⁺, Cu²⁺, Zn²⁺ and Ni²⁺). The presence of culture medium RPMI 1640 at >1% leads to signal reduction due to the presence of excess biotin and iron in this medium. MEM, which lacks these components, does not affect AlphaScreen assays.

Warnings

dBET1 is a thalidomide-derivative, which is known to cause severe birth defects in humans. It is very important to use all appropriate precautions when handling this compound.

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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PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding

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