A cell-permeable, bisphosphonate derivative that displays nanomolar activity against MMP-2 (IC50=37nM), with good selectivity over MMP-8 (320nM), MMP-9 (>1uM), and MMP-14 (> 1uM). It is shown to inhibit osteoclast activity in a macrophage cell line, J774 (IC50=1.7uM), which is more potent compared with other bisphosphonates such as Alendronate, (IC50=30uM), and Zolendronate (7.8uM), without observable cytotoxicity in HepG2 cells. At 25uM, 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.
Chemical Formula:C13H14ClNO8P2S
Solubility:DMSO
Molecular Weight:441.72
Storage and Stability:Store at 4°C. Caution: Light-sensitive. Following reconstitution, aliquot and freeze at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
