FK-506, >99% F-4900
M.W. 804.02 C
M.I. 14: 9025
Storage: Store at or below -20 °C. 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
• Ascomycin level is less than 0.5%.
• Available in gram to kilogram quantities—request a bulk quote.
• FK-506 is a potent immunosuppressant and in vitro T cell
proliferation blocker. It has been shown to disrupt calcineurin
(also known as phosphatase 2B)-mediated signal transduction in
T lymphocytes. The compound interacts with its FK-506-binding
protein-12 (FKBP-12). The resulting complex, in turn, interferes
with calcineurin substrate interaction. Dumont, F.J., “FK-506, 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 aldosteronestimulated Na+ transport and Na(+)-K(+)-ATPase activity. Unlike
rapamycin, which also binds to FK-506-binding protein-12,
FKBP12 with or without bound FK-506 has no effect on rat
brain PKC activity in vitro. McCall, E., “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 aldosteronestimulated 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).
• The CAS number for the anhydrous form of FK-506 is given
above. The CAS number for FK-506 monohydrate is 109581-93-3.
• FK-506 (Tacrolimus) is the active ingredient in the drugs sold
under the trade names Fujimycin® and Prograf®. NOTE: the FK-
506 (Tacrolimus) sold by LC Laboratories is NOT Fujimycin® nor
Prograf® and is NOT for human use.
• Sold for laboratory or manufacturing purposes only; not for
human, medical, veterinary, food, or household use.
• See also our other standard immunosuppresent products:
- Cyclosporin (Cat. No. C-6000 on page 27)
- Everolimus (Cat. No. E-4040 on page 43)
- Rapamycin (Cat. No. R-5000 on page 101)
- Temsirolimus (Cat. No. T-8040 on page 118)
- Zotarolimus, Free Base (Cat. No. Z-9040 on page 134)