FK-506

Tacrolimus, Fujimycin
Calcineurin (PP-2B) Inhibitor-Immunosuppressant
    Cat #: F-900
    Alternative Name Tacrolimus, Fujimycin
  • Lyophilized Powder
  • Bioassay Tested
  • Origin Streptomyces tsukubaensis.
    Source Natural
    MW: 804.03
    Purity: >98%
    Effective concentration 10 pM - 50 nM.
      • FK-506
    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.
      • Fruman, D.A. et al. (1992) Proc. Natl. Acad. Sci. U.S.A. 89, 3686.
      • Cardenas, M.E. et al. (1998) Trends Biotechnol16, 427.
      • Kino, T. et al. (1987) J. Antibiot40, 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.
      • FK-506
        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 Proc23, 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.
      • 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

    Last update: 01/07/2019

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

    For research purposes only, not for human use
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