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Description
General description
An ethyl analog of FK506 with similar immunosuppressant properties. Acts by binding to immunophilins. Inhibits the synthesis of Th-1 and Th-2 type cytokines in target cells.
Ethyl analog of FK-506 that possesses the same potent immunosuppressive properties as the parent compound. Inhibition of the Ca2+/calmodulin activated phosphatase calcineurin (IC50 = 10 nM) by the ascomycin/FK-506 binding protein complex is believed to be important in the mechanism of immunosuppression. Acts by binding immumophilins.
Packaging
1 mg in Plastic ampoule
Biochem/physiol Actions
Cell permeable: no
Fully active via yeast rotamase (FK 506 binding protein) inhibition
Primary Target
Immunophilins
Product does not compete with ATP.
Reversible: no
Warning
Toxicity: Harmful (C)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Ethanol stock solutions are stable for up to 3 days at -20°C. Anhydrous DMSO stock solutions are stable for up to 1 month -20°C.
Other Notes
Paul, C., et al. 2000. Expert Opin. Invest. Drugs9, 69.
Kawai, M., et al. 1993. FEBS Lett.316, 107.
Pilot-Matias, T.J., et al. 1993. Gene128, 219.
Shafiee, A., et al. 1993. J. Antibiot.46, 1397.
Petros, A.M., et al. 1992. J. Med. Chem. 35, 2467.
- Related Categories Cell Biology, Cell Signaling and Neuroscience, Immune Cell Signaling and Blood, Immune System Regulation, Immunomodulators and Antibiotics More... Quality Level