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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. "Effects of FK-506 on contraction and Ca2+ transients in rat cardiac myocytes." Circ. Res. 79: 1110-1121 (1996). Rokaw, M.D., et al. "FK-506 and rapamycin but not cyclosporin inhibit aldosterone-stimulated sodium transport in A6 cells." Am. J. Physiol. 271: C194-202 (1996). Rokaw, M.D., et al. "Rapamycin inhibits protein kinase C activity and stimulates Na+ transport in A6 cells." J. Biol. Chem. 271: 32468-32473 (1996).
Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
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