PROTAC® Optimization Kit for BET Bromodomain-Von Hippel Lindau (VHL) Binding

Products from BPS Bioscience require a minimum order value above 400€

Applications: Great for identifying and optimizing PROTACs targeting BET family of bromodomains, design of novel molecules targeting VHL, and comparison of activities of different PROTACs.

Contraindications: Green and blue dyes that absorb light in the AlphaScreen signalemission range (520-620 nm), such as Trypan Blue. Avoid the use of the potent singlet oxygenquenchers such as sodium azide (NaN3) or metal ions (Fe2+, Fe3+, Cu2+, Zn2+ and Ni2+). Thepresence of culture medium RPMI 1640 at >1% leads to signal reduction due to the presence ofexcess biotin and iron in this medium. MEM, which lacks these components, does not affectAlphaScreen assays.

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.

Storage Stability: At least six months from date of receipt when stored as directed.

Supplied As: The PROTAC Optimization Kit for BET Bromodomain-VHL Binding comes in a convenient AlphaLISA® format, with ARV-771 PROTAC, purified BRD3(BD2) and VHL proteins, and buffer for 384 reactions. (+)JQ1 is included as a control inhibitor of PROTAC binding to BRD

Biosafety Level: Not applicable (BSL-1)

References: Fisher, S.L., Phillips, A.J. Curr Opin Chem Biol 2018; 44:47-55

• Artikelnummer: BPS79790
• Hersteller: BPS Bioscience
• Hersteller Artikelnummer: 79790
• Green Labware: Nein
• Verpackungseinheit: 384 rxns.
• Mengeneinheit: PAK