Merck
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553210

Sigma-Aldrich

Rapamycin - CAS 53123-88-9 - Calbiochem

Rapamycin, CAS 53123-88-9, is an immunosuppressant that selectively inhibits mTOR and blocks the subsequent activation of p70 S6 kinase (IC₅₀ = 50 pM).

Synonym(s):
Rapamycin - CAS 53123-88-9 - Calbiochem, mTOR Inhibitor I
Empirical Formula (Hill Notation):
C51H79NO13
CAS Number:
Molecular Weight:
914.17
MDL number:
NACRES:
NA.77

Quality Level

assay

≥99% (HPLC)

form

film

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

clear

solubility

DMSO: 200 mg/mL
ethanol: 50 mg/mL

shipped in

ambient

storage temp.

−20°C

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 p110Rb phosphorylation, p34cdc2 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 p110Rb phosphorylation, p34cdc2 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.

Packaging

5, 10 mg in Glass bottle
1 mg in Plastic ampoule
100 μg in Plastic ampoule

Biochem/physiol Actions

Target IC50: 50 pM against p70 S6 kinase
Product does not compete with ATP.
Primary Target
Mammalian target of rapamycin (mTOR)
Reversible: no
Cell permeable: no

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

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.

Legal Information

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

Pictograms

Health hazard

Signal Word

Warning

Hazard Statements

Hazard Classifications

Carc. 2 - Repr. 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 2

Certificate of Analysis

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Certificate of Quality

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