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Cyclosporin A

CsA, Ciclosporin

An Immunosuppressant and an Inhibitor of Protein Phosphatase 2B

Cat #: C-900
Alternative Name CsA, Ciclosporin
Lyophilized Powder yes
  • Bioassay Tested
  • Origin Tolypocladium inflatum.
    Source Natural
    MW: 1202.64
    Purity: >99%
    Effective concentration 10-500 nM.
    Molecular formula C62H111N11O12.
    CAS No.: 59865-13-3
    Activity Cyclosporin A is an immunosuppressant and inhibits calcineurin (PP-2B), IC50 = 5 nM1,2.
    1. Fruman, D.A. et al. (1992) Proc. Natl. Acad. Sci. U.S.A89, 3686.
    2. Cardenas, M.E. et al. (1998) Trends Biotechnol16, 427.
    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 or ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or six months at -20°C.
    Our bioassay
    • Alomone Labs Cyclosporin A inhibits the anti-adipogenic effect of calcineurin in 3T3-L1 cells.
      Alomone Labs Cyclosporin A inhibits the anti-adipogenic effect of calcineurin in 3T3-L1 cells.
      Cells were induce to undergo differentiation with 1 μg/ml insulin for 4 days (A, B and C). The cells were treated for the first 4 days of differentiation with 1 µM Ionomycin (#I-700), (B-D) in the presence of 10 ng/ml (C) or 50 ng/ml (D) Cyclosporin A (#C-900). After 10 days, the cells were stained with Oil red O and visualized with light microscopy.
    References - Scientific background
    1. Heitman, J. et al. (1992) New Biol. 4, 448.
    2. Breuder, T. et al. (1994) Proc. Natl. Acad. Sci. U.S.A. 91, 5372.
    3. Cunningham, K.W. and Fink, G.R. (1994) J. Cell Biol. 124, 351.
    4. Cardenas, M.E. et al. (1998) Trends Biotechnol. 16, 427.
    5. Guerini, D. (1997) Biochem. Biophys. Res. Commun. 235, 271.
    6. Schreiber, S.L. and Crabtree, G.R. (1992) Immunol. Today 13, 136.
    7. Graef, I.A. et al. (2001) Cell 105, 863.
    8. Cyert, M.S. et al. (1991) Proc. Natl. Acad. Sci. U.S.A. 88, 7376.
    9. Ye, R.R. and Bretscher, A. (1992) Eur. J. Biochem. 204, 713.
    10. Cyert, M.S. and Thorner, J. (1992) Mol. Cell. Biol. 12, 3460.
    11. Horsley, V. and Pavlath, G.K. (2002) J. Cell Biol. 156, 771.
    12. Flanagan, W.M. et al. (1991) Nature 352, 803.
    13. Clipstone, N.A. and Crabtree, G.R. (1992) Nature 357, 695.
    14. O'Keefe, S.J. et al. (1992) Nature 357, 692.
    15. Ruqin, K. et al. (2002) J. Biol. Chem. 277, 29669.
    16. Andres, D. et al. (2001) Biochem. Pharmacol. 61, 427.
    17. Perry, S.S. et al. (1999) Cell Transplant. 8, 339.
    18. Tavares, P. et al. (1998) J. Cardiovasc. Pharmacol. 31, 46.
    19. Twentyman, P.R. et al. (1992) Br. J. Cancer. 65, 335.
    20. Esposito, C. et al. (2000) Kidney Int. 58, 123.
    21. Nickoloff, B.J. et al. (1988) Am. J. Pathol. 131, 12.
    22. Bell, A. et al. (1994) Biochem Pharmacol. 48, 495.
    Scientific background

    Cyclosporin A is a hydrophobic, cyclic peptide isolated from Tolypocladium inflatum and is a potent immunosuppressant and antifungal compound. It acts via its ability to bind a family of intracellular proteins, the cyclophilins (intracellular peptidyl-prolyl cis-trans isomerases), which are abundant, ubiquitous, highly conserved, and found in multiple forms in different intracellular compartments.1 In yeast, Cyclophilin A, an 18-kDa cytoplasmic protein, mediates Cyclosporin A actions.2,3

    The immunosuppressive action of Cyclosporin A is mediated by the Cyclosporin A-Cyclophilin complex that specifically inhibits the Ca2+/calmodulin-dependent serine-threonine-protein phosphatase-2B (Calcineurin).4-10 This, in turn, inhibits Calcineurin and promotes dephosphorylation of transcription factor NF-AT and T cell activation.11-14 In vivo, Cyclosporin A-induced hypertension involves the attenuation of endothelium-derived NO production through the inhibition of Calcineurin-sensitive pathways regulating eNOS dephosphorylation.15

    Cyclosporin A has been shown to alter cell proliferation in different systems. For hematopoietic progenitor stem and progenitor cells, smooth muscle cells, and hepatocytes, it serves as an inducer of cell proliferation or as a tumor promoting effector.16-18 On the other hand, growth of interleukin-3-dependent mast cells, human lung-cancer cells, tubular kidney cells, cultured pituitary cells, T-cells, and keratinocytes were inhibited by Cyclosporin A.19-21 Moreover, Cyclosporin A has been observed in vitro and in vivo as an antimalarial agent, but the exact mechanism is not yet clear.22

    Last update: 12/08/2021

    Cyclosporin A (#C-900) is a highly pure, natural, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background

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