PROTAC® Optimization Kit for PARP1-Cereblon Binding

The PROTAC® Optimization Kit for PARP1-Cereblon Binding is designed for the testing and profiling of PROTACs directed against PARP1 (Poly (ADP-ribose) -polymerase 1) and Cereblon. The PROTAC® Optimization Kit for PARP1-Cereblon Binding comes in a convenient AlphaLISA® format, with enough PARP1 Degrader iRucaparib-AP6 PROTAC®, assay buffer, recombinant purified PARP1 and CRBN (Cereblon) / DDB1 (damage specific DNA binding protein 1) /Cul4A (cullin 4A) / Rbx1 (ring-box 1) complex for 384 reactions. The PARP1 inhibitor Rucaparib is included as a control inhibitor of PROTAC binding to PARP1 (internal control) .Figure 1. Schematic representation of PARP1-Cereblon complex formation via iRucaparib-AP6 (PROTAC®) .The PROTAC® of interest is incubated with CRBN and PARP1, bringing them in close proximity. PARP1 contains a GST tag, which is recognized by the GSH donor bead. CRBN contains a FLAG tag that binds to the AlphaLISA™ acceptor bead, which is conjugated with 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 and emits light proportionally to the level of interactionNeed us to run inhibitor screens or profile your compounds against PROTAC® Optimization for PARP1-Cereblon Binding? Check out ourPARP/PARPTrap™ Screening ServicesorPROTACs ® & Protein Degradation Services.