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].

参考文献:
[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.