| 货号 | 9974S |
| 供应商 | CST |
| 背景 | 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). |
| 存放说明 | -20C |
| 参考文献 | 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. |
Dose response inhibition of IL-2 secretion by FK-506 in Jurkat cells treated overnight with TPA (40 nM) and A23187 (2 μM). | |
Structure of FK-506 |
