553210

Rapamycin

≥95% (HPLC), powder

• Sinonimo/i: Rapamycin, mTOR Inhibitor I
• Formula empirica (notazione di Hill): C₅₁H₇₉NO₁₃
• Numero CAS: 53123-88-9
• Peso molecolare: 914.17
• Numero MDL: MFCD00867594
• Codice UNSPSC: 41116107
• NACRES: NA.77

Proprietà

• Livello qualitativo: 200
• Saggio: ≥95% (HPLC)
• Stato: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: clear
• Solubilità: DMSO: 200 mg/mL; ethanol: 50 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C
• InChI: QFJCIRLUMZQUOT-UQKHEJQMSA-N

Descrizione

Descrizione generale

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.

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.

Azioni biochim/fisiol

Cell permeable: no

Primary Target
Mammalian target of rapamycin (mTOR)

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50 pM against p70 S6 kinase

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Pittogrammi: GHS08
• Avvertenze: Warning
• Indicazioni di pericolo: H351,H361fd
• Consigli di prudenza: P201 - P202 - P280 - P308 + P313 - P405 - P501
• Classi di pericolo: Carc. 2 - Repr. 2
• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2