NSC 405020

NSC 405020

Catalog Number:
L002368976APE
Mfr. No.:
APE-A4051
Price:
$206
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      • Overview
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          Background

          NSC-405020 is a novel small molecule inhibitor of membrane type-I matrix metalloproteinase (MT1-MMP) that specifically targets the hemopexin (PEX) domain rather than the catalytic domain of MT1-MMP with 50% inhibition concentration IC50 value larger than 100 μmol/L and does not inhibit the catalytic activity of MT1-MMP or MMP-2. 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.

      • Properties
        • Alternative Name
          NSC405020, NSC-405020; 3,4-dichloro-N-pentan-2-ylbenzamide
          CAS Number
          7497-07-6
          Molecular Formula
          C12H15Cl2NO
          Molecular Weight
          260.16
          Appearance
          A solid
          Purity
          99.13%
          Solubility
          insoluble in H2O; ≥11.4 mg/mL in DMSO; ≥96.4 mg/mL in EtOH
          Storage
          Store at RT

          * For Research Use Only

      • Reference
        • 1. Patricia Llorente, Soraia Martins, et al. "Matrix Metalloproteinase 14 Mediates APP Proteolysis and Lysosomal Alterations Induced by Oxidative Stress in Human Neuronal Cells." Oxid Med Cell Longev. 2020 Nov 16;2020:5917187. PMID:33282112
          2. El Azzouzi K, Wiesner C, Linder S. "Metalloproteinase MT1-MMP islets act as memory devices for podosome reemergence." J Cell Biol. 2016 Apr 11;213(1):109-25. PMID:27069022

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