R-5000 Rapamycin, >99%

[RAPA] [Rapamune] [Sirolimus] [AY-22989] [LCP-Siro] [SILA 9268A]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO or ethanol (up to about 50 mg/mL for either solvent).  Disposal:  A

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• Immunosuppressant, related to FK-506, but without calcineurin inhibitory activity even when complexed to FK-506 binding protein.  Selectively blocks signaling that leads to p70 S6 kinase activation (IC50 = 50 pM).  Terada, N., et al.  "Failure of rapamycin to block proliferation once resting cells have entered the cell cycle despite inactivation of p70 S6 kinase."  J. Biol. Chem. 268:  12062-12068 (1993).  Fingar, D.C., et al.  "Dissociation of pp70 ribosomal protein S6 kinase from insulin-stimulated glucose transport in 3T3-L1 adipocytes."  J. Biol. Chem. 268:  3005-3008 (1993).  Price, D.J., et al.  "Rapamycin-induced inhibition of the 70-kilodalton S6 protein kinase."  Science 257:  973-977 (1992).  Chung, J., et al.  "Rapamycin-FKBP specifically blocks growth-dependent activation of and signaling by the 70 kd S6 protein kinases."  Cell 69:  1227-1236 (1992).

• Lymphokine-induced cell proliferation at the G1 phase is inhibited and apoptosis in a murine B cell line is induced by rapamycin.  Rapamycin arrests the Saccharomyces cerevisiae cell cycle irreversibly in the G1 phase.  Morice, W.G. ,et al.  "Rapamycin-induced inhibition of p34cdc2 kinase activation is associated with G1/S-phase growth arrest in T lympho