Catalog number: 232 - M5630
Product Category: Business & Industrial > Science & Laboratory
Size: 1EA
79924
The PROTAC Optimization Kit for CDK Kinase-Cereblon Binding is designed for testing and profiling of PROTACs directed against the CDK Kinase 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.<br /><br />The CDK inhibitor Palbociclib is included as a control inhibitor of PROTAC binding to CDK. 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 CDK4 or CDK6 Kinase. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.
78420
The PROTAC Optimization Kit for BRD9-Cereblon Binding is designed for the testing and profiling of PROTACs directed against BRD9 and Cereblon (CRBN). The BRD9 inhibitor BI-7273 is included as a control inhibitor of PROTAC binding to BRD9. With this kit, three simple steps are required for the measurement of PROTAC activity. First, the PROTAC of interest is incubated with CRBN and BRD9. Next, acceptor beads are added, then donor beads, followed by reading of the Alpha-counts.Illustration of the assay principle: a PROTAC of interest or positive control dBRD9 (PROTAC) interacts with both BRD9 and CRBN, bringing them in close proximity. BRD9 contains a GST tag, recognized by the GSH donor bead, while CRBN contains a FLAG tag that binds to the AlphaLISA™ acceptor bead conjugated with an anti-FLAG antibody. Upon excitation of the donor bead a singlet oxygen is generated by the donor bead, which excites the acceptor bead and emits light proportionally to the level of interaction. AlphaLISA™ immunoassays are a no-wash alternative to ELISA immunoassays. These assays are robust and ideal for a minimal hands-on approach.
78441
The PROTAC Optimization Kit for PARP1-Cereblon Binding is designed for the testing and profiling of PROTACs directed against PARP1 and Cereblon (CRBN). This Kit comes in a convenient AlphaLISA™ format, with the PARP1 Degrader iRucaparib-AP6 (PROTAC) added as positive control, PARP1 buffer, purified PARP1 and CRBN proteins for 384 reactions. The PARP1 inhibitor Rucaparib is included as a control that blocks PROTAC binding to PARP1. With this kit, three simple steps are required for the measurement of PROTAC activity. First, the PROTAC of interest is incubated with CRBN and PARP1. Next, acceptor beads are added, then donor beads, followed by reading of the Alpha-counts.Illustration of the assay principle: A PROTAC of interest or positive control iRucaparib-AP6 (PROTAC) interacts with both PARP1 and CRBN, bringing them in close proximity. PARP1 contains a GST tag, recognized by the GSH donor bead, while CRBN contains a FLAG tag that binds to the AlphaLISA™ acceptor bead 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 interaction. AlphaLISA™ immunoassays are a no-wash alternative to ELISA immunoassays. These assays are robust and ideal for a minimal hands-on approach.