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. The PROTAC Optimization Kit for BET Bromodomain-Cereblon Binding comes in a convenient AlphaLISA(R) 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.