MMP-2/MMP-9 Inhibitor I

- Overview
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    Background
    
    IC50: 310 and 240 nM for MMP-2 and MMP-9, respectivelyMMP-2/MMP-9 Inhibitor I is a potent inhibitor of matrix metalloproteinase-2 (MMP-2) and MMP-9.Matrix metalloproteinase (MMP), a typical metalloproteinase, requires zinc ion at its active sites. As many as 18 kinds of MMP have been identified and cloned and are collectively called the MMP family. In vitro: MMP-2/MMP-9 inhibitor I was identified as a potent inhibitor of matrix metalloproteinase-2 (MMP-2) and MMP-9 with IC50 values of 310 and 240 nM, respectively. MMP-2/MMP-9 inhibitor I acted by binding zinc at the active site of these MMPs. MMP-2/MMP-9 inhibitor I was found to be able to block MMP-2/MMP-9-dependent invasion in cell culture model [1].In vivo: Both hydroxamic acid and carboxylic acid analogs of MMP-2/MMP-9 inhibitor I were evaluated for their inhibitory activities in animal cancer models. Results showed that lung colonization of Lewis lung carcinoma cells was suppressed by these inhibitors significantly. In addition, antitumor activity was also observed in the human lung cancer model. Ma44 cells growed as a solid tumor on the peritoneum after being implanted ip, and mice bearing Ma44 eventually died within 3 to 4 weeks. Daily oral administration of compound 5l led to prolonged survival of Ma44-bearing mice [1].Clinical trial: So far, no clinical study has been conducted.
- Properties
  - Alternative Name
    
    Metalloproteinase-2/Metalloproteinase-9 Inhibitor I; N-([1,1'-biphenyl]-4-ylsulfonyl)-D-phenylalanine
    
    CAS Number
    
    193807-58-8
    
    Molecular Formula
    
    C21H19NO4S
    
    Molecular Weight
    
    381.4
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤25mM in DMSO
    
    Storage
    
    Store at 4°C
    
    * For Research Use Only

MMP-2/MMP-9 Inhibitor I

Background

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