NSC 405020

NSC 405020 binds to the hemopexin (PEX) domain of the membrane type-1 matrix metalloproteinase (MT1-MMP/MMP-14).{34792} It disrupts MT1-MMP homodimerization without affecting its catalytic activity in an assay using the MT1-MMP CAT domain, which is involved in its tumor promoting function (IC50 > 100 µM). In a mouse tumor xenograft model, it reduces tumor growth through a cell death-independent mechanism when injected intratumorally at a dose of 0.5 mg/kg three times per week for two weeks. NSC 405020 (1 µM) applied to HSC5 cells prevents arsenic-mediated invasion while also decreasing the expression of MT1-MMP and pERK.{34793}