Overview
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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.
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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
FK-506 (#F-900) is a highly pure, natural, and biologically active compound.
Applications
Citations
Powered by Bioz- Ulrich, J.D. et al. (2012) J. Biol. Chem. 287, 37594.
