Product Pathways - Translational Control
Rapamycin (FRAP/mTOR Inhibitor) #9904
Directions for Use
Rapamycin is supplied as a lyophilized powder. For a 100 µM stock, resuspend 10 nmol (9.1 µg) in 100 µl methanol or DMSO.
Description
Rapamycin is soluble in DMSO and methanol. For experiments with cultured cells, CST recommends pretreating with 10 nmol of this inhibitor for one hour prior to stimulation.
Background
Rapamycin is a bacterial macrolide with antifungal and immunosuppressant activities (1). Rapamycin forms a complex with the immunophilin FKBP12 which then inhibits the activity of FRAP/ mTOR (TOR in yeast) (2,3). Rapamycin treatment of cells leads to the dephosphorylation and inactivation of p70 S6 kinase. Rapamycin also leads to the dephosphorylation of 4E-BP1/PHAS1, thereby promoting its binding to and inactivation of eIF4E (4,5). This activity has been shown to be the basis for Rapamycin's ability to block protein synthesis and to arrest cell cycle progression in the G1-phase (6,7). However, it has been suggested that Rapamycin's inhibition of the G1/S transition may be the consequence of its effect on cyclin D1 mRNA and protein stability (8).
Rapamycin is soluble in DMSO and methanol. For experiments with cultured cells, CST recommends pretreating with 10 nmol of this inhibitor for one hour prior to stimulation.
- Dumont, F. J. et al. (1990) J. Immunol. 144, 251-258.
- Brown, E. J. et al. (1994) Nature 369, 756-758.
- Kunz, J. et al. (1993) Cell 73, 585-596.
- Jefferies, H. B. et al. (1997) EMBO J. 15, 3693-3704.
- Beretta, L. et al. (1996) EMBO J. 15, 658-664.
- Thomas, G. and Hall, M.N. (1997) Curr. Opin. Cell. Biol. 9, 782-787.
- Dennis, P. B. et al. (1999) Curr. Opin. Genet. & Develop. 9, 49-54.
- Hashemolhosseini, S. et al. (1998) J. Biol. Chem. 273, 14424-14429.
Application References
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This product is for in vitro research use only and is not intended for use in humans or animals. This product is not intended for use as therapeutic or in diagnostic procedures.