Targeted Protein Degradation Services
Accelerate the discovery and development of degrader molecules with our comprehensive screening and profiling services.
- Comprehensive Services: Utilize cutting-edge technologies for robust data.
- Expert Collaboration: Work closely with our team to design customized experiments.
- Advanced Platforms: Leverage our experience in Targeted Protein Degradation.
- Tailored Solutions: Address unique challenges with specialized support.
- Insightful Results: Drive your project forward with reliable data and insights.
Whether you are exploring novel degraders or optimizing existing candidates, our services will deliver the results you need. Learn more about our services below or contact us for details.
Degradation Compound Profiling Services
Endpoint Degradation Profiling
Ideal for screening large compound libraries
- Single concentration or dose response to determine DC50
- Multiple time points to assess fast (5–6 hours) and sustained (18–24 hours) degradation
- Cell viability multiplex
Kinetic Degradation Profiling
Ideal for ranking kinetic parameters of hit degraders
- Single concentration or dose response monitored for 24 hours
- Analysis of degradation rate, Dmax and Dmax50 against concentration to evaluate kinetic potency
- Endpoint cell viability multiplex
Endogenously Tagged HiBiT Neosubstrate Panel to Enable Molecular Glue Discovery
Six neosubstrate targets for IMiD molecular glues were established as HiBiT CRISPR knock-in cell lines across different cell types: IKZF1 and IKZF2 (Jurkat), IKZF3 (MM.1S), SALL 4 (SK-N-DZ), CK1α and GSPT1 (HEK293). This neosubstrate panel enables screening for molecular glue library degradation selectivity and off-target effects with CRBN-recruiting PROTACs. Recommended endpoints for screening include 6 and 24 hours, with concurrent cell viability counter-screen. RLU values were normalized to CellTiter-Glo® Luminescent Cell Viability Assay.
Permeability and Affinity Services
NanoBRET® Target Engagement and Cellular Permeability
- De novo assay and tracer development
- Assessment of degrader binding affinity to target and E3
- Assessment of degrader permeability in live vs permeabilized cells
Degrader Results with Automated VHL TE Assay
Panel A. Compound concentration-response curves from NanoBRET® TE VHL assays in live-cell or permeabilized-cell modes, respectively. VH298 was used as a permeable control compound. Panel B. Lower and upper asymptote, IC50, and Hill slope parameters calculated from non-linear regression curves.
VHL TE Assay Permeability Parameters
Calculated relative binding affinity (RBA) and availability index (AI) values for each compound. An RBA value of approximately 1 indicates similar free concentrations inside and outside of the cell. AI > 1 suggests reduced availability inside the cell compared to VH298 control. AI < 1 could indicate compound accumulates in cells at higher relative concentrations compared to VH298 control.
Ternary Complex Formation Services
NanoBRET® Ternary Complex Formation
- De novo assay development and testing
- Degrader profiling in endpoint or kinetic format
- Single concentration or dose response
Screening for Neosubstrate Ternary Complex Formation with Transient NanoBRET® Assay
NanoBRET® Ternary Complex Assay optimization for common neosubstrates and CRBN. NanoLuc® neosubstrate and HaloTag® CRBN fusions were expressed in HEK293 cells with or without protease inhibitor MG132. All N- and C- orientations were tested at 1:10 and 1:100 ratios. Results show a significant increase in BRET upon addition of molecular glue due to formation of ternary complex.
Ubiquitination Services
NanoBRET® Target Ubiquitination
- De novo assay development and testing
- Degrader profiling in endpoint or kinetic format
- Single concentration or dose response
Custom Services
Learn how our custom services can support your research and development efforts.
- Development of Innovative Cell Lines: Get cell lines using Promega reporter technology, specifically engineered to your specifications.
- Custom Assay Development: Assays meticulously designed to test and validate your compounds, streamlining your research process.
- Advanced Tools and Expertise: With access to our cutting-edge technologies, our experts will work with you to get the results you need.