F-4900 FK-506, >98%
M.W. 804.02 C44H69NO12 [104987-11-3]
Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 100 mg/mL; soluble in ethanol at 100 mg/mL; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Disposal: A
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Ascomycin level is less than 0.5%.
FK-506 is a potent immunosuppressant and in vitro T cell proliferation blocker. It has been shown to disrupt calcineurin (also known as CaN or phosphatase 2B)-mediated signal transduction in T lymphocytes. The compound interacts with its FK506-binding protein-12 (FKBP12). The resulting complex, in turn, interferes with calcineurin substrate interaction. Dumont, F.J. "FK506, an immunosuppressant targeting calcineurin function." Curr. Med. Chem. 7: 731-748 (2000).
FK-506 inhibits FKBP activity resulting in an increase in the release of sarcoplasmic reticulum-derived calcium. FK-506 also appears to inhibit Na(+)-Ca2+ exchange. Prolonged exposure of Xenopus A6 cells to FK-506 significantly inhibits aldosterone-stimulated Na+ transport and Na(+)-K(+)-ATPase activity. Unlike rapamycin, which also binds to FK506-binding protein-12, FKBP12 with or without bound FK506 has no effect on rat brain PKC activity in vitro. McCall, E., et al.