Biochem/physiol Actions

Cell permeable: no

Reversible: no

Primary TargetFarnesyl diphosphate synthase

Product does not compete with ATP.

Target IC₅₀: 460 nM against farnesyl diphosphate synthase; ~ 40 - 70 µM as as a broad-spectrum MMP inhibitor; ~ 1 pM against in vitro invasion of prostate cancer cells

General description

An amino-bisphosphonate that acts as a potent inhibitor of bone resorption and cartilage destruction. Causes disruption of the ruffled border and actin cytoskeleton of osteoclasts and induces in vitro apoptosis of osteoclasts and macrophages by inhibiting farnesyl diphosphate synthase (IC₅₀ = 460 nM). Efficiently chelates metal ions and functions as a broad-spectrum MMP inhibitor (IC₅₀ ~ 40 - 70 µM). Also displays antimetastatic, anti-invasive and cell-adhesion-promoting properties (IC₅₀ ~ 1 pM, in vitro invasion of prostate cancer cells).

An amino-bisphosphonate that acts as a potent inhibitor of bone resorption and cartilage destruction. Causes disruption of the ruffled border and actin cytoskeleton of osteoclasts. Shown to induce apoptosis of osteoclasts and macrophages. Inhibits farnesyl disphosphate synthase (IC₅₀ = 460 nM with purified enzyme and 1.7 µM with cell extracts). Also shown to inhibit migration, cell adhesion, and invasion of cells (IC₅₀ = 1 pM in prostate cancer cell invasion assays). Efficiently chelates metal ions and functions as a matrix metalloprotease (MMP) inhibitor (IC₅₀ = 40-70 µM).

Legal Information

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

Other Notes

Lehenkari, P.P., et al. 2002. Mol. Pharmacol.62, 1255.Virtanen, S.S., et al. 2002. Cancer Res.62, 2708.Bergstrom, J.D., et al. 2000. Arch. Biochem. Biophys.373, 231.Smith, R., et al. 1971. Lancet1, 945.Fleisch, H., et al. 1969. Nature223, 211.

Packaging

100 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Harmful (C)