Biotin-Ahx-Ub-VS

a potent and specific inhibitor of deubiquitinating enzymes (DUBs), labeled with biotin on the N-terminus

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Description

Biotin-Ahx-Ub-VS (UbiQ-188) is a potent and specific inhibitor of deubiquitinating enzymes (DUBs) based on a C-terminal electrophilic vinyl sulfone (VS) group. UbiQ-188 can be used for activity profiling experiments and determining DUB inhibitor specificity. It is labeled on the N-terminus with a biotin and an aminohexanoic acid (Ahx) linker is introduced to create extra space between the biotin and Ub protein for efficient access of biotin binding entities. To eliminate Met1 oxidation, Met1 is replaced by norleucine, a well validated Met mimic.

Galardy, P., et al. Mechanism-based proteomics tools based on ubiquitin and ubiquitin-like proteins: crystallography, activity profiling, and protease identification. Methods in Enzymology. 399, 120-131 (2005).
http://www.ncbi.nlm.nih.gov/pubmed/16338352

de Jong, A., et al. Ubiquitin-based probes prepared by total synthesis to profile the activity of deubiquitinating enzymes. ChemBiochem 13, 2251-2258 (2012).
http://www.ncbi.nlm.nih.gov/pubmed/23011887

Wrigley, J.D. et al. Enzymatic characterisation of USP7 deubiquitinating activity and inhibition. Cell Biochem. Biophys. 60, 99-111 (2011)
http://www.ncbi.nlm.nih.gov/pubmed/21468692