Rapamycin

  • 来源:上海康成生物工程有限公司
  • 时间: 2008/1/30
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    Rapamycin

    FRAP/mTOR

     

    Catalog No: KC-4R001

    Size: 1 mg

     

     

    Physical Appearance:  Off-white or yellow solid

     

    Molecular Formula:  C51H79NO13

     

    Molecular Weight:  914.2

     

    Purity:  98% (TLC: 10% MeOH/Methylene chloride; Rf = 0.51)

     

    Solubility:  Soluble in DMSO (25 mg/ml)

     

    Storage:  Store, as supplied, at –20°C for up to 1 year. Store solutions at -20°C for up to 3 months.

     

    Background:  Rapamycin is a bacterial macrolide with antifungal and immunosuppressant activities. Rapamycin forms a complex with the immunophilin FKBP12 which then inhibits the activity of FRAP/mTOR (TOR in yeast). Rapamycin treatment of cells leads to the dephosphorylation and inactivation of p70 S6 kinase. Rapamycin also leads to the dephosphorylation of 4E-BP1/PHAS1, thereby promoting its binding to and inactivation of eIF4E. This activity has been shown to be the basis for Rapamycin’s ability to block protein synthesis and to arrest cell cycle progression in the G1-phase. However, it has been suggested that Rapamycin’s inhibition of the G1/S transition may be the consequence of its effect on cyclin D1 mRNA and protein stability.

     

    Description:  Description: Rapamycin (FRAP/mTOR) is soluble in DMSO and methanol. For use with in vitro or cell based assays, it may be diluted into aqueous buffers to yield desired concentrations with final DMSO concentrations of ~0.1%. IC50 values for inhibitory activity against FRAP/mTOR are around 50 pM. Such inhibitory activity is seen in cultured cells stimulated with fetal calf serum or a variety of growth factors. For experiments with cultured cells, CST recommends pretreating with 10 nM of this inhibitor for one hour prior to stimulation.

     

    References:

    1.      J.Y.Chang et al. Trends Pharmacol.Sci. 1991 12 218

    2.      J.Choi et al. Science 1996 273 183

    3.      D.M.Sabatini et al. J.Biol.Chem. 1995 270 20875

    4.      E.J.Brown et al. Nature 1995 377 441

    5.      J.E.Kay et al. Immunology 1991 72 544

    6.      W.G.Morice et al. J.Biol.Chem. 1993 268 3734

    7.      J.Heitman et al. Science 1991 253 905

    8.      D.J.Price et al. Science 1992 257 973

    9.      D.C.Fingar et al. J.Biol.Chem. 1993 268 3005

    10.    J.Chung et al. Cell 1992 69 1227

     

    The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.

     

     

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