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Rapamycin

RAPA, Rapamune, Sirolimus, AY-22989, NSC-226080
An Immunosuppresant, Anticancer Compound, and Protein Phosphatase Inhibitor
Cat #: R-900
Alternative Name RAPA, Rapamune, Sirolimus, AY-22989, NSC-226080
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Streptomyces hygroscopicus subsp. hygroscopicus.
    Source Natural
    MW: 914.2
    Purity: >99%
    Effective concentration 1-20 nM.
    Structure
    Chemical name (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34 aS)9,10,12,13,14,21,22,23,24,25,26,27,32,33,34,34a-Hex adecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4- hydro xy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy- 6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c] [1,4]oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)- pentone.
    Molecular formula C51H79NO13.
    CAS No.: 53123-88-9.
    Activity Rapamycin is an antifungal antibiotic with immunosuppressive activities1. It can inhibit calcineurin when in complex with FKBP122. Rapamycin also exhibits anticancer properties3.
    References-Activity
    1. Cardenas, M. et al. (1994) Perspect. Drug Discov. Des2, 103.
    2. Fruman, D.A. et al. (1992) Proc. Natl. Acad. Sci. U. S. A89, 3686.
    3. Edinger, A.L. et al. (2003) Cancer Res63, 8451.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO, methanol. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Rapamycin inhibits the proliferation of WEHI B lymphocyte cells.
      Alomone Labs Rapamycin inhibits the proliferation of WEHI B lymphocyte cells.
      Cells were treated with different concentrations of Rapamycin (#R-900) for 4 days; the number of live cells was measured by XTT cell proliferation assay kit, normalized to the control (100%) and plotted against the drug concentration.
    References - Scientific background
    1. Cardenas, M. et al. (1994) Perspect. Drug Discov. Des. 2, 103.
    2. Albers, M. et al. (1993) J. Biol. Chem. 268, 22825.
    3. Aimee L. Edinger, et al. (2003) Cancer Res63, 8451.
    4. Hosoi, H. et al. (1999) Cancer Res59, 886.
    5. Huang, S. et al. (2001) Cancer Res61, 3373.
    6. Liu, J. et al. (1991) Cell 66, 807.
    7. Fruman, D. A. et al. (1992) Proc. Natl. Acad. Sci. U. S. A. 89, 3686.
    Scientific background

    Rapamycin is a natural macrocyclic antibiotic with both antifungal and immunosuppressive activities.1 In mammalian T-lymphocytes, Rapamycin blocks the signal transduction pathway initiated by interleukin-2.2

    Rapamycin has also shown promising anticancer activities in preclinical and clinical studies,3 acting as an antiproliferative agent in vascular, endothelial and smooth muscle cells. It also induced apoptosis in two rhabdomyosarcoma cell lines.4

    Together with FKBP12, Rapamycin creates a toxic complex that irreversibly inhibits mTOR kinase- a downstream effector of the phosphatidylinositol 3-kinase/Akt signaling pathway.3,5 By the use of this mechanism Rapamycin arrests the progression of G-phase T-cells to S phase.6 The FKBP12 -Rapamycin complex also inhibits the Ca2+-calmodulin-regulated protein serine-threonine phosphatase, Calcineurin.7

    Last update: 22/09/2020

    Rapamycin (#R-900) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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