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).
- 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.
Molecular Formula
C51H79NO13
Molecular Weight
914.17 g/mol
Purity
>99%
CAS
53123-88-9
Solubility
Soluble in DMSO at 200mg/ml and EtOH at 50mg/ml.
Storage
Directions for Use
Rapamycin is supplied as a lyophilized powder. For a 100 µM stock, resuspend 10 nmol (9.1 µg) in 100 µl ethanol or DMSO. For experiments with cultured cells, CST recommends pretreating with 10 nM of this inhibitor for one hour prior to stimulation.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
Limited Uses
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