We hereby announce the launch of an activity-based probe that is designed to selectively target USP7: K58K(biotin) cRh110-Cys-Ubv(USP7)-PA (UbiQ-314).

UbiQ-314 is based on Ub with the following mutations: T7D, L8Y, I13R, E34L, Q40N, L69A, and L71A. Residue Lys58 contains a biotin tag which, besides detection and binding, also serves to increase USP7 selectivity by prohibiting binding of most USPs. The N-terminus is functionalised with a 5-carboxyrhodamine110 dye (cRh110, λex = 480 nm; λem = 520 nm) allowing for a sensitive and fast (in-gel fluorescence) detection. A Cys residue is introduced between the dye and N-terminus for further modification with thiol-reactive tags. In addition, UbiQ-314 contains a C-terminal propargyl amide (PA, also sometimes abbreviated as Prg) warhead, which forms a covalent linkage with the active site Cys residue of USP7 and can be cleaved by acid treatment (5% aq. TFA), allowing for proteomic analyses.

references:

Gjonaj et al. Chem Comm 2019, 55, 5075: https://pubs.rsc.org/en/content/articlelanding/2019/cc/c9cc00969h

Mandal et al. Angew Chem Int Ed Engl 2021, 60, 7333: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8048964/

Ekkebus et al. J Am Chem Soc. 2013, 135, 2867: http://www.ncbi.nlm.nih.gov/pubmed/23387960

Sommer et al. Bioorg Med Chem 2013, 21, 2511: https://pubmed.ncbi.nlm.nih.gov/23535560/

For additional information, to download the product sheet and to order, please see UbiQ-314