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We offer a variety of services to support targeted protein degradation research, including cell line generation, assay development, screening and profiling services. Learn more about our services below or contact us for details.

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Degradation Compound Profiling Services Using Endogenous HiBiT Targets

18802ma

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
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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
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Endogenously Tagged HiBiT Neosubstrate Panel to Enable Molecular Glue Discovery

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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. CC-885 displays broad selectivity, while DKY709 shows robust degradation of IKZF2 and SALL4.


Services for Mechanistic Evaluation and Optimization of Degrader Efficacy

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
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Degrader Results with Automated VHL TE Assay

vhl-live-ic50-results
vhl-perm-ic50-results

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

vhl-te-assay-permeability-parameters-table

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.


NanoBRET® Ternary Complex Formation

  • De novo assay development and testing
  • Degrader profiling in endpoint or kinetic format
  • Single concentration or dose response
18803ma
brd2-crbn

Screening for Neosubstrate Ternary Complex Formation with Transient NanoBRET® Assay

18811ma
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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.


NanoBRET® Target Ubiquitination

  • De novo assay development and testing
  • Degrader profiling in endpoint or kinetic format
  • Single concentration or dose response
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