FK-506 #9974
Product Information
Product Usage Information
FK-506 is supplied as a 10 mg powder. Store at -20ºC. FK-506 is soluble in DMSO and EtOH at 100mg/ml, and stock solutions should be stored at -20ºC. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used between 1 and 10 nM.
Storage
Product Description
| Molecular Weight | 804.02 g/mol |
| Purity | >99% |
| Molecular Formula | C44H69NO12 |
| CAS | 104987-11-3 |
| Solubility | Soluble in DMSO and EtOH at 100mg/ml. |
Background
The calcium dependent protein phosphatase calcineurin is responsible for the de-phosphorylation of the transcriptional regulator nuclear factor of activated T cells (NFAT) and is essential for NFAT’s nuclear translocation and activation (1,2). Calcineurin is a target of two common immunosuppressants, cyclosporin A (CsA) (3) and FK-506 (also know as tacrolimus and fugimycin) (4), both of which can inhibit antigen and mitogen triggered T cell activation. These drugs interact with the immunophilins cyclophilin and FKBP-12, respectively, and the immunophilin-drug complex binds to calcineurin to inhibit substrate binding (5). FK-506 can be up to 100-fold more potent than CsA in various models (6-8).
- Schulz, R.A. and Yutzey, K.E. (2004) Dev Biol 266, 1-16.
- Rusnak, F. and Mertz, P. (2000) Physiol Rev 80, 1483-521.
- Borel, J.F. et al. (1976) Agents Actions 6, 468-75.
- Kino, T. et al. (1987) J Antibiot (Tokyo) 40, 1249-55.
- Liu, J. et al. (1991) Cell 66, 807-15.
- Henderson, D.J. et al. (1991) Immunology 73, 316-21.
- Tocci, M.J. et al. (1989) J Immunol 143, 718-26.
- Yoshimura, N. et al. (1989) Transplantation 47, 351-6.
Limited Uses
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