Description
General description
A potent, selective, slow-binding and mechanism-based inhibitor of human gelatinases, MMP-2 (Ki = 13.9 nM) and MMP-9 (Ki = 600 nM). It also exhibits a covalent mechanism based behavior in inhibition of these enzymes. This inhibitor appears to have similarity to TIMP-1 and TIMP-2 in the slow-binding component of inhibition. Shown to directly bind to the zinc in the catalytic site of MMP-2. Does not affect the activities of MMP-1 (Ki = 206 µM) MMP-3 (Ki = 15 µM), or MMP-7 (Ki = 96 µM).
Biochem/physiol Actions
Product does not compete with ATP.
Reversible: no
Cell permeable: no
Packaging
Packaged under inert gas
Other Notes
Krüger, A., et al. 2005. Cancer Res.65, 3523.
Kleinfeld, O., et al. 2001. J. Biol. Chem.276, 17125.
Brown, S., et al. 2000. J. Am. Chem. Soc.122, 6799.
Legal Information
Sold under license of U.S. Patent 6,703,415.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)