Rapamycin 是一种特异性的 mTOR 抑制剂，IC50 为 0.1 nM。 抗真菌剂和免疫抑制剂。选择性抑制哺乳动物雷帕霉素靶蛋白(mTOR)，并阻断随后的p70 S6激酶激活(IC50 = 50 pM)。可特异性抑制mTORC1，但可磷酸化Akt（蛋白激酶B）Ser473位的mTORC2则对雷帕霉素不敏感。防止 IGF-II 的翻译激活。还防止静止的T细胞进入细胞周期，但不直接阻止细胞周期进程。研究表明，可抑制随后的信号传导事件，例如p110Rb 磷酸化、p34cdc2激酶激活和细胞周期蛋白A合成。表现出与FK-50 6结合蛋白的强结合力。还据报道在鼠B细胞系中诱导凋亡，抑制淋巴因子诱导的细胞增殖（在G1期），并不可逆地阻滞酿酒酵母细胞（在G1）。 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.