FK-506 (Tacrolimus, Fujimycin)
|Biochemicals||Storage: 4°C/-20°CShipping: Blue Ice|
Potent immunosuppressant (as cyclosporin A and rapamycin). Suppresses proliferation of cytotoxic T cells and inhibits the production of T cell-derived mediators such as interleukin-2 (IL-2). Forms a complex with FK-506 binding protein 12 (FKBP12). Inhibits the activity of the calcium/calmodulin-dependent protein phosphatase 2B (PP2B; calcineurin), leading to disruption of T cell activation. Prevents rejection of transplanted organs. Anti-inflammatory compound in the treatment of several inflammatory skin diseases (e.g. atopic dermatitis) and with potential anti-rheumatic activity (rheumatoid arthritis). Neuroprotective. Regulates nitric oxide neurotoxicity. Neurotransmitter. Ca2+ release compound. NF-kappaB suppressor by induction of unfolded protein response (UPR). Anti-cancer compound. Apoptosis inducer.
Storage and Stability:
Short-term Storage: +4°C
Long-term Storage: -20°C
Stable for at least 2 years after receipt when stored at -20°C.
C44H69NO12 . H2O
Important Note: This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
FK-506, a novel immunosuppressant isolated from a Streptomyces. I. Fermentation, isolation, and physico-chemical and biological characteristics: T. Kino, et al.; J. Antibiot. (Tokyo) 40, 1249 (1987)
Cyclosporin A, FK506 and rapamycin: more than just immunosuppression: J. Kunz & M.N. Hall; TIBS 18, 334 (1993)
Cyclosporin A and FK506: molecular mechanisms of immunosuppression and probes for transplantation biology: B.E. Bierer, et al.; Curr. Opin. Immunol. 5, 763 (1993)
The actions of cyclosporin A and FK506 on T-lymphocyte activation: P.S. Mattila; Biochem. Soc. Trans. 24, 45 (1996) (Review)
FK506 in the treatment of inflammatory skin disease: promises and perspectives: G. Michel, et al.; Immunol. Today 17, 106 (1996) (Review)
The mechanism of action of cyclosporin A and FK506: S. Ho, et al.; Clin. Immunol. Immunopathol. 80, S40 (1996) (Review)
FK506, an immunosuppressant targeting calcineurin function: F.J. Dumont; Curr. Med. Chem. 7, 731 (2000) (Review)
FK506 and its analogs - therapeutic potential for neurological disorders: A. Klettner & T. Herdegen; Curr. Drug Targets CNS Neurol. Disord. 2, 153 (2003) (Review)
A review of the action of tacrolimus (FK506) on experimental models of rheumatoid arthritis: S. Miyata, et al.; Inflamm. Res. 54, 1 (2005) (Review)
Metabolism of tacrolimus (FK506) and recent topics in clinical pharmacokinetics: K. Iwasaki; Drug Metab. Pharmacokinet. 22, 328 (2007) (Review)
Suppression of NF-kappaB by cyclosporin A and tacrolimus (FK506) via induction of the C/EBP family: implication for unfolded protein response: S. Du, et al.; J. Immunol. 182, 7201 (2009)
FK506 binding proteins as targets in anticancer therapy: S. Romano, et al.; Anticancer Agents Med. Chem. 10, 651 (2010) (Review)