General Description
An oxirane analog of SB-3CT, pMS (Cat. No. 444285) that acts as a selective, active site-binding, irreversible inhibitor of MMP-2 (Ki = 2.4 μM). Although less potent, it exhibits enhanced selectivity towards MMP-2 (Ki = 45 and 379 μM for MMP-1 and MMP-7, respectively) than SB-3CT, pMS.
Biological Activity
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].
Biochem/physiol Actions
Secondary TargetMMP-2 (Ki = 45 and 379 μM for MMP-1 and MMP-7, respectively)
References
[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.
