Fig. 2 | Scientific Reports

Fig. 2

From: The small molecule LOXL2 inhibitor SNT-5382 reduces cardiac fibrosis and achieves strong clinical target engagement

Fig. 2

SNT-5382 is an irreversible, mechanism-based inhibitor of LOXL2. (A) Chemical structure of SNT-5382. (B) The potency of human recombinant LOXL2 activity by SNT-5382 increases with pre-incubation. (n = 3). (C) The irreversible binding of SNT-5382 measured in a jump dilution assay for both human recombinant (hr) LOXL2 and LOXL1. The reversible inhibitor is the des-fluoro analogue of SNT-5382. (n = 3). (D) Concentration response curves of the inhibition of lysyl oxidase family enzymatic activity had a 30 min pre-incubation and measured using an Amplex Red oxidation assay, as described previously29; hn: human native; hr: human recombinant. (n = 3). (E) Postulated mechanism of inhibition of SNT-5382. Data are presented as mean ± SD.

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