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 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.Need us to run inhibitor screens or profile your compounds against PROTAC® Optimization for BET Bromodomain-Von Hippel Lindau (VHL) Binding? Check out ourBromodomain Screening ServicesorPROTACs ® & Protein Degradation Services.

Product Specifications

Format

Catalog #ComponentAmountStorage100373VHL Complex, FLAG-tag25 µg-80°CAvoid freeze/thaw cycles31033BRD3 (BD2), GST-tag10 µg-80°CARV-771 (MW = 987 Da) 10 µg-80°C793113x Immuno Buffer 14 ml-20°C27403 (+) -JQ1 (10 mM) 20 µg-20°C*The initial concentrations of VHL and BRD3 are lot specific and will be indicated on the tubes containing the proteins

Shipping Conditions

-80°C

Storage Conditions

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

Contraindications

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