Merck, 553211-1MG, Rapamycin

General description
Selectively inhibits the phosphorylation and activation of p70 S6 kinase (IC₅₀ = 50 pM). 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.
Biochem/physiol Actions
Cell permeable: no
Primary Target
Mammalian target of rapamycin (mTOR)
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 50 pM inhibiting the mammalian target of rapamycin (mTOR) and blocking the subsequent activation of p70 S6 kinase
Packaging
Packaged under inert gas
Physical form
2.5 mg/mL solution in DMSO (2.74 mM)
Preparation Note
Following initial use, aliquot and freeze (-20°C).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)