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.