PROTAC Optimization Kit for BET Bromodomain-Cereblon Binding
1658.92 €
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Catalog number: 421 - 79770
Product Category: Business & Industrial > Science & Laboratory
Gentaur
Size: 384 rxns.
79790
PROTAC Optimization Kit for BET Bromodomain-Von Hippel Lindau (VHL) Binding
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<br />detection. First, a sample containing PROTAC is incubated with VHL and BRD3(BD2), one of the<br />BET bromodomains. Next, acceptor beads are added, then donor beads, followed by reading the Alpha-counts.
1454.40 €
79924
PROTAC Optimization Kit for CDK Kinase-Cereblon Binding
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.
1454.40 €
78420
PROTAC® Optimization Kit for BRD9-Cereblon Binding
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.
1454.40 €