ARP 100

Matrix metalloproteinases (MMPs) belong to a family of proteases that play a crucial role in tissue remodeling and repair by degrading extracellular matrix proteins to enable cell migration.¹ During cancer progression both MMP-2 and MMP-9 play a role in metastatic tumor dispersion and angiogenesis. ARP 100 is a biphenylsulfonamide that acts as a selective inhibitor of MMP-2 demonstrating an IC₅₀ value of 12 nM.^2,3 Due to its specific zinc binding domain configuration, the inhibitory activity of ARP 100 is significantly less potent towards MMP-1, MMP-3, MMP-7, and MMP-9 (IC₅₀ values are 50, 4.5, 50, and 0.2 µM, respectively).^2,3 At 50 nM, ARP 100 suppresses the invasive behavior of HT1080 tumor cells grown on matrigel.²

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1. Nagase, H., and Woessner, J.F., Jr. Matrix metalloproteinases. The Journal of Biological Chemisty 274(31), 21491-21494 (1999).

2. Rossello, A., Nuti, E., Orlandini, E., et al. New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg. Med. Chem. 12(9), 2441-2450 (2004).

3. Tuccinardi, T., Martinelli, A., Nuti, E., et al. Amber force field implementation, molecular modelling study, synthesis and MMP-1/MMP-2 inhibition profile of (R)- and (S)-N-hydroxy-2-(N-isopropoxybiphenyl-4-ylsulfonamido)-3-methylbutanamides. Bioorg. Med. Chem. 14(12), 4260-4276 (2006).