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Beschreibung

An orally active non-peptidyl hydroxamate compound that acts as an effective broad-spectrum inhibitor against MMP-2/3/8/9/12/13 (Ki = 0.73, 42, 1.1, 2.1, 0.45, and 1.1 nM, respectively), but not MMP-1 (IC50 = 1.6 µ,M), MMP-7 (Ki = 2.5 µ,M), or other serine proteases (no activity against chymotrypsin or plasmin at 100 µ,M). Widely used in studying MMP-mediated diseases development in vivo. Also reported to block P-LAP secretase activity (>=70% inhibition of P-LAP shedding at 10 µ,M) that is otherwise not inhibited by TIMP-1/2 in CHO cell cultures in vitro., An orally active non-peptidyl hydroxamate compound that acts as an effective broad-spectrum inhibitor against MMP-2, -3, -8, -9, -12, -13 (Ki = 0.73, 42, 1.1, 2.1, 0.45, and 1.1 nM, respectively), but not MMP-1 (IC50 = 1.6 µ,M), MMP-7 (Ki = 2.5 µ,M), or other serine proteases (no activity against chymotrypsin or plasmin at 100 µ,M). Widely used in studying MMP-mediated diseases development in vivo. Also reported to block P-LAP secretase activity (>=70% inhibition of P-LAP shedding at 10 µ,M) that is otherwise not inhibited by TIMP-1/2 in CHO cell cultures in vitro.