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Beschreibung

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-beta3/MT tumor growth in xenografted mice (0.5 mg/kg, intratumoral).