Merck, 444295-25MG, MT1-MMP Inhibitor, NSC405020

General description
A cell-permeable pentanylbenzamide compound that acts as an allosteric, reversible, and selective inhibitor of the collgenolytic activity of MT1-MMP. Does not affect the catalytic activity of cellular MT-1-MMP thus allows it to retain its ability to activate MMP-2. Selectively targets the hemopexin (PEX) domain of MT1-MMP, thereby repressing its pro-tumorigenic activity. Its binding to the PEX domain is dependent on Met-328, Arg-330, Asp-376, Met-422, and Ser-470 in the druggable pocket of the enzyme. Shown to block 184B5-MT cell migration on collagen-1 and repress MCF7-β3/MT tumor growth in xenografted mice (0.5 mg/kg, intratumoral).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 year at -20°C.
Other Notes
Remacle, A.G., et al. 2012. Cancer Res.72, 2339.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)