MMP-2 Inhibitor IV

A cell-permeable, bisphosphonate derivative that displays nanomolar activity against MMP-2 (IC₅₀ = 37 nM), with good selectivity over MMP-8 (320 nM), MMP-9 (>1 M), and MMP-14 (>1 M). It is shown to inhibit osteoclast activity in a macrophage cell line, J774 (IC₅₀ = 1.7 M), which is more potent compared with other bisphosphonates such as Alendronate (Cat. No. 126855), (IC₅₀ = 30 M), and Zolendronate (7.8 M), without observable cytotoxicity in HepG2 cells. At 25 M, it abolishes the formation of actin rings, which are functional structures that are typical of resorbing osteoclasts, at activity levels comparable with those of zolendronic acid, inhibits bone resportion in vitro, and demonstrates cytotoxic properties in murine osteoclasts.

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Rubino, M.T., et al. 2011. Chem. Med. Chem.6, 1258.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany