553210

Rapamycin

≥95% (HPLC), powder

• Synonym(s): Rapamycin, mTOR Inhibitor I
• Empirical Formula (Hill Notation): C₅₁H₇₉NO₁₃
• CAS Number: 53123-88-9
• Molecular Weight: 914.17
• UNSPSC Code: 41116107
• NACRES: NA.77
• MDL number: MFCD00867594

Properties

• Product Name: Rapamycin, ≥95% (HPLC), powder
• InChI key: QFJCIRLUMZQUOT-UQKHEJQMSA-N
• assay: ≥95% (HPLC)
• form: powder
• 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
• Quality Level: 200

Description

Biochem/physiol Actions

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50 pM against p70 S6 kinase

Cell permeable: no

Primary Target
Mammalian target of rapamycin (mTOR)

Disclaimer

Toxicity: Standard Handling (A)

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.

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.

Preparation Note

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

Legal Information

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

Safety Information

• pictograms: GHS08
• signalword: Warning
• hcodes: H351,H361fd
• pcodes: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Hazard Classifications: Carc. 2 - Repr. 2
• Storage Class: 11 - Combustible Solids
• wgk: WGK 2