General description

An orally active non-peptidyl hydroxamate compound that acts as an effective broad-spectrum inhibitor against MMP-2/3/8/9/12/13 (K_i = 0.73, 42, 1.1, 2.1, 0.45, and 1.1 nM, respectively), but not MMP-1 (IC₅₀ = 1.6 µM), MMP-7 (K_i = 2.5 µM), or other serine proteases (no activity against chymotrypsin or plasmin at 100 µM). 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 µM) 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 (K_i = 0.73, 42, 1.1, 2.1, 0.45, and 1.1 nM, respectively), but not MMP-1 (IC₅₀ = 1.6 µM), MMP-7 (K_i = 2.5 µM), or other serine proteases (no activity against chymotrypsin or plasmin at 100 µM). 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 µM) that is otherwise not inhibited by TIMP-1/2 in CHO cell cultures in vitro.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Okamoto, Y., et al. 2007. Int. Heart J.48, 369.Ito, N., et al. 2004. Biochem. Biophys. Res. Commun.314, 1008.Shiraga, M., et al. 2002. Cancer Res.62, 5967.Mori, T., et al. 2001. Exp. Biol. Med.226, 429.Yamada, A., et al. 2000. Inflamm. Res.49, 144.

Packaging

2 mg in Plastic ampoule

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)