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. 2014 Mar 16;5(5):1352–1362. doi: 10.18632/oncotarget.1817

Figure 1. Identification of novel small molecule Hepsin inhibitors.

Figure 1

(A) Attenuation of Hepsin-dependent proteolytic activity by the lead compound #4 [20] and its derivatives. Purified recombinant Hepsin was preincubated with 2 μM of the indicated compounds for 30 min. The residual percent activity of the enzyme toward the chromogenic substrate was determined using a microplate reader at 405 nm. Data are the means of three independent experiments ±SD. (B) IC50 determination for Hepsin inhibitors #4, HepIn-1, HepIn-8, HepIn-13, HepIn-17, HepIn-20, HepIn-25. Data are the means of three independent experiments ±SD. (C) Chemical structures of identified Hepsin inhibitors.