Immunosuppressive agents such as cyclosporin A, FK506, and rapamycin are used routinely in clinical transplantation and the treatment of autoimmune disorders. Cyclosporin A and FK506 bind to cyclophilins and the FK-binding protein FKBP12, respectively. These complexes interact with, and inhibit the activity of, the calcineurin protein phosphatase, which is essential for T cell activation. Rapamycin also interacts with FKBP12, but this complex does not affect calcineurin. Instead, it inhibits signals required for G1 to S progression in yeast, in IL-2-stimulated T lymphocytes, and other mammalian cell types. Rapamycin-FKBP12 binds to a protein designated Rapamycin And FKBP12 Target-1 (RAFT1) in rats and FKBP-Rapamycin-Associated Protein (FRAP) in humans. RAFT1 is the homolog of the yeast genes TOR1 and TOR2 which, when mutated, lead to rapamycin resistance. RAFT1 is a PI4-kinase that exhibits homology with other PI kinases such as PI3-kinase and PI4-Kα. RAFT1 phosphorylates p70 S6 kinase and 4E-BP1 which are regulators of translational initiation. However, rapamycin-FKBP1 does not inhibit PI4-kinase activity and, therefore, affects RAFT1 activity via alternate mechanisms.
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注意事项：
1.Since applications vary, each investigator should titrate the reagent to obtain optimal results.
2.Caution: Sodium azide yields highly toxic hydrazoic acid under acidic conditions. Dilute azide compounds in running water before discarding to avoid accumulation of potentially explosive deposits in plumbing.
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