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Launch of an activity-based probe designed to selectively target USP7.

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 (Gjonaj et al.). 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, exc/emi 480/520 nm) allowing for 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. 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 of USP7 that can be cleaved by acid treatment (5% aq. TFA), allowing for proteomic analyses.

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

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