Rapamycin

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.

Primary Target
Mammalian target of rapamycin (mTOR)

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50 pM against p70 S6 kinase

Cell permeable: no

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

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

Toxicity: Standard Handling (A)