Merck, 342500-5MG, FK-506, Streptomyces sp.

General description
Immunosuppressant that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 binding protein, thereby reversing its effects on sarcoplasmic reticulum Ca²⁺ release. Inhibits the Ca²⁺-dependent phosphatase, Protein Phosphatase 2B (Calcineurin; Cat. No. 539568), as well as Na⁺,K⁺-ATPase in nephron segments. Also shown to inhibit aldosterone-induced synthesis of Giα-3 protein.
Immunosuppressant that blocks T-cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 Binding Protein, thereby reversing its effects on sarcoplamic reticulum Ca²⁺ release. Shown to inhibit the Ca²⁺-dependent phosphatase, Calcineurin (Cat. No. 539565), as well as Na⁺-K⁺-ATPase in nephron segments. Also shown to inhibit aldosterone-induced synthesis of Giα-3 protein.
Biochem/physiol Actions
Cell permeable: no
Primary Target
Immunosuppressant that blocks T cell proliferation
Product does not compete with ATP.
Reversible: no
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Asano, K., et al. 1996. In Vivo 10, 537.
McCall, E., et al. 1996. Circ. Res. 79, 1110.
Raufman, J.P., et al. 1996. J. Biol. Chem. 271, 19877.
Rokaw, M.D., et al. 1996. Am. J. Physiol. 271, C194.
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Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Toxic (F)