Description: 71431-30-6

Description: JBS True Blue

Description: 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.

Description: The PROTAC Optimization Kit for IRAK4-Cereblon Binding is designed for the testing and profiling of PROTACs directed against IRAK4 and Cereblon (CRBN). The IRAK4 ligand-1 is included as a control that blocks PROTAC binding to IRAK4. With this kit, only three simple steps are required for the measurement of PROTAC activity. First, the PROTAC of interest is incubated with CRBN and IRAK4. 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 IRAK4 Degrader-1 (PROTAC) interacts with both IRAK4 and CRBN, bringing them in close proximity. IRAK4 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.

Description: 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.

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.

Description: 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._x000D_ The PROTAC Optimization Kit for BET Bromodomain-Cereblon Binding comes in a convenient AlphaLISA® 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._x000D_

Description: The PROTAC Optimization Kit for BET Bromodomain-Von Hippel Lindau (VHL) Binding is designed for testing and profiling PROTACs directed against the BET Bromodomain family and VHL complex. VHL is a substrate recognition component of E3 protein ligase complex and is linked by Elongin C to a heterodimeric Cul2/Rbx1 module, which functions as a potent activator of the ubiquitination of target proteins by an E2 conjugating enzyme. Elongin B interacts with the complex through Elongin C and stabilizes the binding of Elongin C to VHL. Mutations in VHL are associated with the inherited von Hippel-Lindau cancer syndrome and numerous forms of renal cell carcinoma. 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 VHL and BRD3(BD2), one of the
BET bromodomains. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.

Description: Thermus aquaticus, recombinant, E. coli