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. 2020 Jul 7;3(8):e202000768. doi: 10.26508/lsa.202000768

Figure 1. FT3967385 is a selective covalent USP30 inhibitor.

Figure 1.

(A) Chemical structure of FT3967385 (FT385). (B) Concentration-dependent inhibition of recombinant USP30 activity using ubiquitin–rhodamine as a substrate. (C) Bio-layer interferometry traces showing no significant off-rate at indicated concentrations. Red line indicates removal of the inhibitor after 180 s. (D) Progress curves characteristic of a covalent inhibitor (0–6.67 μM), these are fitted to obtain KI and kinact. (E) Data table of inhibitory properties. (F) DUB specificity screen (DUB profiler; Ubiquigent) with 2, 20, and 200 nM FT385.