NSC-405020 (7497-07-6) is a membrane type-1 matrix metalloproteinase (MMP14 or MT1-MMP) inhibitor that prevents homodimerization and inhibits MMP14’s protumorigenic activity?in vivo. (IC50?> 100 μM). Inhibition is via interaction with the hemopexin domain (PEX) of MMP14. NSC-405020 does not interfere with the catalytic activity of MT1-MMP or MMP-2.? Suppresses bone erosion in a c-Fos-deficient mouse model.2?Decreases arsenic-mediated invasion of human squamous cell carcinoma HSC5 cells.3
NSC 405020 is a novel, selective, and noncatalytic membrane type-1 matrix metalloproteinase (MT1-MMP) inhibitor that directly interacts with the homopexin (PEX) domain of MT1-MMP.
1) Remacle?et al.?(2012),?Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth;? Cancer Res.,?72?2339
2) Kittaka?et al.?(2018)?Cherubism Mice Also Deficient in c-Fos Exhibit Inflammatory Bone Destruction Executed by Macrophages That Express MMP14 Despite the Absence of TRAP+ Osteoclasts?; J. Bone Miner. Res.,?33?167
3) Thang?et al.?(2014)?Bidirectional functions of arsenic as a carcinogen and an anti-cancer agent in human squamous cell carcinoma; PLoS One,?9(5)?e96945
