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Questions about a product, technology or experimental design? Give us a call 610-644-8845.

E3 TR-FRET Biochemical Assay

Advanced high-throughput screening solutions for E3 ligase drug discovery powered by our proprietary TUBE technology

E3 ligases remain among the most difficult enzyme targets to assay and discover potent therapeutic applications, possibly due to their dependence on upstream E1 and E2 enzymes for the activation and transfer of ubiquitin. As a result, traditional assays for E3 ligases are complex and prone to off-target false positives.

At LifeSensors, we have developed reagents and assays encompassing both traditional and non-traditional approaches for E3 ligase screening and profiling. Quickly distinguishing true hits from false positives, developing structure-activity relationships, and establishing rank order potency from purified enzymes to cellular models are key steps to success. LifeSensors brings together the tools and expertise necessary to overcome the many pitfalls in the E3 ligase field.

Our E3 TR-FRET detection system utilizes our TUBE technology to monitor E3 ligase activity by fluorescence signal. This assay involves donor-labeled TUBEs that bind to acceptor-labeled polyubiquitin chains synthesized by the target E3 ligase. When donor-labeled TUBEs come in close proximity to polyubiquitin chains containing acceptor-labeled ubiquitin will yield in a FRET signal. This signal can be monitored over time in a homogenous, high-throughput format, making it ideal for small-molecule screening to find tool compounds for E3 ligases.

Homogenous Format

No wash steps required

Real-Time Monitoring

Continuous signal tracking

High-Throughput

Ideal for screening
Comprehensive E3 ligase screening capabilities

High-Throughput Screening

Using compound libraries to discover novel inhibitors/activators/binders for E3 ligases

Automated Liquid Handling

Amenable to large library screening with precision and efficiency

Extensive E3 Ligase Access

~50 E3 ligases available for discovery and selectivity studies in rapid homogenous assay format

Customized Compound Libraries

Access to ligase-centric small molecule libraries for reference in drug discovery efforts

Ultrasensitive Detection

Robust signal-to-noise ratio powered by proprietary TUBE technology

Extensive UPS Experience

Complementary biochemical and biophysical validation studies to exclude off-target hits

Unlocking the Impact of E3 Ligases in Drug Discovery

Comprehensive guide to E3 ligase targeting and screening methodologies

Complete assay kits for enzyme activity measurement

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UC-0106

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UC-0201

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Recombinant enzymes for ubiquitination studies

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