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-b3/MT tumor growth in xenografted mice (0.5mg/kg, intratumoral).
Formula:C₁₂H₁₅Cl₂NO
Solubility:DMSO
Molecular Weight:260.2
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
