Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product does not compete with ATP.

Primary TargetMammalian target of rapamycin (mTOR)

Target IC₅₀: 50 pM against p70 S6 kinase

General description

Selectively inhibits the mammalian target of rapamycin (mTOR) and blocks the subsequent activation of p70 S6 kinase (IC₅₀ = 50 pM). Specifically inhibits mTORC1, but mTORC2 that phosphorylates Akt at Ser⁴⁷³ appears to be insensitive to rapamycin. Prevents the translational activation of IGF-II. Also prevents resting T-cells from entering the cell cycle, but does not directly arrest cell cycle progression. Shown to inhibit later signaling events, such as p110^Rb phosphorylation, p34^cdc2 kinase activation, and cyclin A synthesis. Exhibits strong binding to FK-506 binding proteins. Also reported to induce apoptosis in a murine B-cell line, to inhibit lymphokine-induced cell proliferation at the G₁ phase, and to irreversibly arrest Saccharomyces cerevisiae cells in the G₁ phase.

Anti-fungal and immunosuppressant. Selectively inhibits the mammalian target of rapamycin (mTOR) and blocks the subsequent activation of p70 S6 kinase (IC₅₀ = 50 pM). Specifically inhibits mTORC1, but mTORC2 that phosphorylates Akt at Ser⁴⁷³ appears to be insensitive to rapamycin. Prevents the translational activation of IGF-II. Also prevents resting T-cells from entering the cell cycle, but does not directly arrest cell cycle progression. Shown to inhibit later signaling events, such as p110^Rb phosphorylation, p34^cdc2 kinase activation, and cyclin A synthesis. Exhibits strong binding to FK-506 binding proteins. Also reported to induce apoptosis in a murine B-cell line, to inhibit lymphokine-induced cell proliferation at the G₁ phase, and to irreversibly arrest Saccharomyces cerevisiae cells in the G₁ phase. A 5 mM (500 µg/109 µl) solution of Rapamycin (Cat. No. 553211) in DMSO and a 10 mM (1 mg/109 µl) solution of Rapamycin (Cat. No. 553212) in EtOH is also available.

Legal Information

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

Other Notes

Chen, T., et al. 2011. Aging Cell.10, 908.Powell, D.J., et al. 2003. Mol. cell Biol.23, 7794.Braun, W., et al. 1995. FASEB J.9, 63.Nielsen, F.C., et al. 1995. Nature 377, 358.Aagaard-Tillery, K.M. and Jelinek, D.F. 1994. Cell. Immunol. 156, 493.Gottschalk, A.R., et al. 1994. Proc. Natl. Acad. Sci. USA91, 7350.Morice, W.G., et al. 1993. J. Biol. Chem.268, 3734.Terada, N., et al. 1993. J. Biol. Chem.268, 12062.Kuo, J., et al. 1992. Nature 358, 70.Price, D.J., et al. 1992. Science257, 973.Heitman, J., et al. 1991. Science253, 905.Kay, J.E., et al. 1991. Immunology72, 544.Schreiber, S.L. 1991. Science251, 283.Bierer, B.E., et al. 1990. Proc. Natl. Acad. Sci. USA87, 9231.Dumont, F.J., et al. 1990. J. Immunol.144, 251.

Packaging

1 mg in Plastic ampoule

5, 10 mg in Glass bottle

100 µg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)