PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding

PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding
Artikelnummer
BPS79770
Verpackungseinheit
384 rxns.
Hersteller
BPS Bioscience

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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.

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. The PROTAC Optimization Kit for BET Bromodomain-Cereblon Binding comes in a convenient AlphaLISA® format, with dBET1 PROTAC, Immuno Buffer 1, and purified BRD3(BD2) and CRBN for 384 reactions. (+)JQ1 is included as a control inhibitor of PROTAC binding to BRD3(BD2). 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 BET bromodomains. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.

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

Supplied As: Great for search of proper PROTACs targeting BET family of bromodomains, design of novel molecules targeting CRBN, and comparison of activities of different PROTACs.

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.

Biosafety Level: Not applicable (BSL-1)

References: Winter, G.E., Paulk, J., Roberts, J.M., et al. Science 2015; 348(6241):1376-81.
Mehr Informationen
Artikelnummer BPS79770
Hersteller BPS Bioscience
Hersteller Artikelnummer 79770
Green Labware Nein
Verpackungseinheit 384 rxns.
Mengeneinheit PAK
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