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FK-506

Tacrolimus, Fujimycin

Calcineurin (PP-2B) Inhibitor-Immunosuppressant

Cat #: F-900
Alternative Name Tacrolimus, Fujimycin
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Streptomyces tsukubaensis.
    Source Natural
    MW: 804.03
    Purity: >98%
    Effective concentration 10 pM - 50 nM.
    Structure
    Chemical name (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11, 12,13,14,15,16,17,18,19,24,25,26,26a Hexadecahydro-5,19 - dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyc lohexyl]-1- methylethenyl]-14,16-dimethoxy-4,10,12,18-te tramethyl-8-(2-propen-1-yl)- 15,19-epoxy-3H-pyrido[2,1-c ][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)tetrone
    Molecular formula C44H69NO12.
    CAS No.: 104987-11-3
    Activity FK-506 is an immunosuppressant and inhibits calcineurin (PP-2B)1-3.
    References-Activity
    1. Fruman, D.A. et al. (1992) Proc. Natl. Acad. Sci. U.S.A. 89, 3686.
    2. Cardenas, M.E. et al. (1998) Trends Biotechnol. 16, 427.
    3. Kino, T. et al. (1987) J. Antibiot. 40, 1249.
    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 FK-506 inhibits the anti-adipogenic effect of calcineurin in 3T3-L1 cells.
      Alomone Labs FK-506 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 and C) in the presence of 5 ng/ml (C) or absence (A and B) of FK-506 (#F-900). After 10 days, the cells were stained with Oil red O and visualized with light microscopy.
    References - Scientific background
    1. Kino, T. et al. (1987) J Antibiot. 40, 1249.
    2. Kino, T. et al. (1987) J Antibiot. 40, 1256.
    3. Goto, T. et al. (1991) Transplant Proc. 23, 2713.
    4. Rosen, M.K. and Schreiber, S.L. (1992) Angew. Chem. Int. Ed. Engl. 31, 384.
    5. Schreiber, S.L. et al. (1992) Immunol Today. 13, 136.
    6. Harding, M.W. et al. (1989) Nature. 341, 758.
    7. Bierer, B. et al. (1990) Science. 250, 556.
    8. Jin, Y. et al. (1991) PNAS 88, 6677.
    9. Schreiber, S.L. et al. (1992) Immunol Today. 13, 136.
    10. Liu, J. et al. (1991) Cell 66, 807.
    11. O'Keefe, S.J. et al. (1992) Nature (London) 357, 692.
    12. Dumont, F.J. et al. (1992) Journal of Experimental Medicine 176, 751.
    13. McCall, E. et al. (1996) Circ. Res. 79, 1110.
    Scientific background

    FK 506 (Tacrolimus), a macrolide compound isolated from Streptomyces tsukubaensis, is a potent immunosuppressive compound that inhibits T-cell activation and is an inhibitor of fungal growth (10 to 100 times more potent than Cyclosporin A).1-3 FK-506 binds and inhibits, in vitro, the activity of immunophilin proteins known as FK 506-binding protein (FKBP), in a variety of organisms, ranging from yeast to humans.4-8

    Immunosuppression activity of FK-506 seems to be due to FK-506/FKBP complex that inhibits the heterodimeric Ca2+/calmodulin-dependent phosphatase Calcineurin. This, in turn, prevents the Calcineurin-dependent activation of interleukin-2 transcription and T-cell proliferation.9-12 FK-506 inhibits FKBP activities, increases sarcoplasmic reticulum Ca2+ release and decreases the ability of Na+/Ca2+ exchange to extrude Ca2+ from the cell.13

    Lyophilized Powder
    Last update: 02/03/2021

    FK-506 (#F-900) is a highly pure, natural, and biologically active compound.

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    For research purposes only, not for human use

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    Scientific Background

    Citations

    Citations
    Product citations
    1. Ulrich, J.D. et al. (2012) J. Biol. Chem. 287, 37594.

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