MK 217

Biological Activity

Osteoclast-mediated bone resorption inhibitor. Binds and blocks farnesyl diphosphate synthase (FPPS) in the HMG-CoA pathway (IC₅₀ = 460 nM for recombinant human FPPS); causes macrophage apoptosis. Inhibits prenylation and sterol biosynthesis in purified osteoclasts.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Alendronate is a specific, nanomolar inhibitor of fanesyl diphosphate synthase.
   Bergstrom et al.
   Arch.Biochem.Biophys., 2000;373:231
2. Lowering bone mineral affinity of bisphosphonates as a therapeutic strategy to optimize skeletal tumor growth inhibition in vitro.
   Fournier et al.
   Cancer Res., 2008;68:8945
3. Alendronate mechanism of action; geranylgeraniol, an intermediate in the mevalonate pathway, prevents inhibition of osteoclast formation, bone resorption, and kinase activation in vitro.
   Fisher et al.
   Proc.Natl.Acad.Sci., 1999;96:133

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