PROTAC® Optimization Kit for BET Bromodomain-Cereblon Binding

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.Need us to run inhibitor screens or profile your compounds against PROTAC® Optimization for BET Bromodomain-Cereblon Binding? Check out ourBromodomain Screening ServicesorPROTACs ® & Protein Degradation Services.This product has beencited 4 times.

Product Specifications

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®.

Format

Catalog #ComponentAmountStorage100329Cereblon/DDB1/Cul4A/ Rbx1 Complex30 µg-80°CAvoid freeze/thaw cycles31033BRD3 (BD2), GST-tag5 µg-80°CdBET1 (1 mM) 10 µl-80°C793113x Immuno Buffer 14 ml-20°C27403 (+) -JQ1 (10 mM) 10 µl-20°C*Concentration of Cereblon and BRD3 will be indicated on the tube containing protein

Shipping Conditions

-80°C

Storage Conditions

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

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.