MMP-2 Inhibitor II

- Overview
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    Background
    
    MMP-2 Inhibitor II is an irreversible, potent and selective MMP-2 inhibitor with Ki value of 2.4 μM [1]. Matrix metalloproteinases (MMPs) are zinc-dependent endopeptidases that play important roles in physiological and pathological conditions. Two MMPs, gelatinases A and B (MMP-2 and MMP-9, respectively), is highly expressed in human cancer, and a direct relationship between cancer progression and gelatinase expression and activity has been well established [1]. MMP-2 Inhibitor II, an oxirane p-sulfonamido analog of SB-3CT, is an irreversible, potent and selective MMP-2 inhibitor. MMP-2 Inhibitor II inhibited MMP-2, MMP-1 and -7 with Ki values of 2.4 μM, 45 and 379 μM, respectively, and didn’t inhibit MMP-3, -7, or -9 [1]. In bovine retinal endothelial cells, MMP-2 Inhibitor II reduced glucose-induced increases in the gelatinolytic activity of MMP-2 and mRNA levels of MMP-2 and MT1-MMP. MMP-2 Inhibitor II also inhibited glucose-induced alterations in TIMP-2 and MT1-MMP gene expressions [2]. MMP-2 Inhibitor II had also been used to examine the role of MMP-2 in rheumatoid synovial fibroblast survival, inflammation, and cartilage degradation [3].
    
    [1]. Ikejiri M, Bernardo MM, Bonfil RD, et al. Potent mechanism-based inhibitors for matrix metalloproteinases. J Biol Chem. 2005 Oct 7;280(40):33992-4002.
    [2]. Kowluru RA, Kanwar M. Oxidative stress and the development of diabetic retinopathy: contributory role of matrix metalloproteinase-2. Free Radic Biol Med. 2009 Jun 15;46(12):1677-85.
    [3]. Xue M, McKelvey K, Shen K, et al. Endogenous MMP-9 and not MMP-2 promotes rheumatoid synovial fibroblast survival, inflammation and cartilage degradation. Rheumatology (Oxford). 2014 Dec;53(12):2270-9.
- Properties
  - Alternative Name
    
    Matrix Metalloproteinase-2 Inhibitor II; N-[4-[4-[(2-oxiranylmethyl)sulfonyl]phenoxy]phenyl]-methanesulfonamide
    
    CAS Number
    
    869577-51-5
    
    Molecular Formula
    
    C16H17NO6S2
    
    Molecular Weight
    
    383.4
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≤200mg/ml in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

MMP-2 Inhibitor II

Background

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