204140-01-2

MMP-9/MMP-13 inhibitor I is a cell-permeable inhibitor of matrix metalloproteinases (MMPs) that most potently inhibits MMP-9 and MMP-13 (IC₅₀s = 0.9 nM for both). It less effectively inhibits MMP-1, MMP-3, and MMP-7 (IC₅₀s = 43, 23, and 920 nM, respectively). MMP-9/MMP-13 inhibitor I has been used to elucidate the roles of MMPs in biological systems, including tumor cell invasion and pathogenesis of P. falciparum.

A piperazine-based, cell-permeable, and highly potent inhibitor of MMP-9 and MMP-13

MMP-9: 0.9 nM (IC₅₀); MMP-13: 0.9 nM (IC₅₀); MMP-1: 43 nM (IC₅₀); MMP-3: 23 nM (IC₅₀); MMP-7: 931 nM (IC₅₀)

[1] MENYAN CHENG. Design and Synthesis of Piperazine-Based Matrix Metalloproteinase Inhibitors[J]. Journal of Medicinal Chemistry, 2000, 43 3: 369-380. DOI: 10.1021/jm990366q
[2] MAURO PRATO. Phagocytosis of hemozoin enhances matrix metalloproteinase-9 activity and TNF-alpha production in human monocytes: role of matrix metalloproteinases in the pathogenesis of falciparum malaria.[J]. Journal of immunology, 2005, 175 10: 6436-6442. DOI: 10.4049/jimmunol.175.10.6436
[3] PETER STORZ. FOXO3a promotes tumor cell invasion through the induction of matrix metalloproteinases.[J]. Molecular and Cellular Biology, 2009, 29 18: 4906-4917. DOI: 10.1128/mcb.00077-09
[4] MUTHULEKHA SWAMYDAS. Mesenchymal stem cell-derived CCL-9 and CCL-5 promote mammary tumor cell invasion and the activation of matrix metalloproteinases.[J]. Cell Adhesion & Migration, 2013, 7 3: 315-324. DOI: 10.4161/cam.25138