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.

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