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).

Legal Information

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

Other Notes

Remacle, A.G., et al. 2012. Cancer Res.72, 2339.

Packaging

25 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 year at -20°C.

Warning

Toxicity: Standard Handling (A)