PROTAC® Optimization Kit for CDK Kinase-Cereblon Binding

The PROTAC® Optimization Kit for CDK-Cereblon Binding is designed for the testing and profiling of PROTACs directed against the CDK (Cyclin-dependent kinase family) and Cereblon. The PROTAC® Optimization Kit for CDK-Cereblon Binding comes in a convenient AlphaLISA® format, with enough BSJ-03-204 PROTAC®, CDK PROTAC® buffer, purified CDK4, CDK6, and CRBN for 384 reactions. The CDK inhibitor Palbociclib is included as a control inhibitor of PROTAC binding to CDK (internal control) .Figure 1. Schematic representation of CDK-Cereblon complex formation via BSJ-03-204 PROTAC®.The PROTAC® of interest is incubated with CRBN and CDK4 or CDK6, bringing them in close proximity. CDK contains an His-tag, which is recognized by the donor bead. CRBN contains a FLAG tag that binds to the AlphaLISA™ acceptor bead, which is conjugated to an anti-FLAG antibody. Upon excitation of the donor bead, a singlet oxygen is generated by the donor bead. The singlet oxygen excites the acceptor bead, which emits light proportionally to the level of interaction