NSC 405020 3,4-Dichloro-N-(1-Methylbutyl)benza-Mide;NSC 405020;3,4-Dichloro-N-(1-methylbutyl)-benzamide NSC405020;NSC 405020 3,4-Dichloro-N-(1-methylbutyl)-benzamide;NSC 405020, >=98% 7497-07-6
NSC-405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 μM and does not inhibit the catalytic activity of MT1-MMP or MMP-2.
IC50 value: > 100 uM [1]
Target: MT1-MMP PEX inhibitor
NSC-405020 directly interacts with and binds to PEX in a vicinity of Met-328, Arg-330, Asp-376, Met-22 and Ser-470 of the druggable pocket in the full-length MT1-MMP structure, which affects the conformation and flexibility of blades I to IV of the β-propeller resulting in the decrease of the PEX-dependent homodimerization of cellular MT1-MMP. NSC-405020 dose not affect the ability of MT1-MMP to activate MMP-2 but its ability to degrade COL-I.
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