DUBprofiler-Cell™: DUB target engagement assay
Determination of DUB inhibitor in-cell target engagement
With the small molecule chemical tractability of DUBs demonstrated by a number of groups through the development of high affinity and selective inhibitors (supported by the DUBprofiler™ service) it is now becoming increasingly important to determine the in-cell DUB target engagement profile of these molecules as these drug discovery programmes progress towards the clinic.
We are now developing such a service with support from key collaborations such as CAST.
DUBprofiler-Cell™ will enable:
- Determination of the DUB target engagement profile of your compound(s) in a live cell environment
- Addressing; physiological protein folding, the cellular milieu for compound target engagement (pH, redox conditions etc), sub-cellular penetration (compound) and localisation (target), post-translational modifications and the presence of subunits, co-factors and substrates
- Single point and EC50 determinations
- Determination of DUB cellular target engagement in the presence and absence of stimuli
- Determination of compound cell penetration
- The capability to interrogate a cell lysate environment if your molecule is not cell penetrant
- Profiling of any cell line and potentially tissues