PROTAC® Optimization Kit for CDK Kinase-Cereblon Binding

The PROTAC® Optimization Kit for Cyclin-dependent kinase (CDK)-Cereblon Binding is designed for the testing and profiling of PROTACs directed against the CDK family and Cereblon. Cereblon (CRBN) is a substrate recognition component of the DCX (DDB1-CUL44-Rbx1) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins.

The PROTAC Optimization Kit for CDK-Cereblon Binding comes in a convenient AlphaLISA® format, with BSJ-03-204 PROTAC, CDK PROTAC buffer, purified CDK4 and CDK6, and CRBN for 384 reactions. The CDK inhibitor Palbociclib is included as a control inhibitor of PROTAC binding to CDK (internal control). With this kit, only three simple steps are required for PROTAC activity detection. First, the PROTAC of interest is incubated with CRBN and CDK4 or CDK6. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.

Figure 1. Schematic representation of CDK-Cereblon complex formation via BSJ-03-204 PROTAC.