FK-506 (CAS 104987-11-3)
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FK-506, also referred to as Tacrolimus, is an immunosuppressant of the macrolide class. It serves as a valuable compound in the research of preventing organ transplant rejection and treating autoimmune diseases, inflammatory bowel diseases, and specific types of cancers. This potent immunosuppressant functions by binding to and inhibiting the enzyme calcineurin, which plays a role in T-lymphocyte activation. In scientific research, FK-506 has found diverse applications. Studies have employed it to investigate the impact of immunosuppression on the immune system and to explore its effects on the development and progression of certain cancers. Furthermore, FK-506 has been utilized in cell culture studies and investigations into gene expression. By binding to and inhibiting calcineurin activity, FK-506 effectively suppresses T-lymphocyte activation, leading to the suppression of the immune response. FK-506 is an agent that binds to the immunophilin FKBP12 and inhibits PP2B (calcineurin). FK-506, cyclosporin A (sc-3503), and rapamycin (sc-3504) have been shown to inhibit specific transduction pathways, which results in T lymphocyte activation. The compound can also inhibit cAMP levels in the presence of carbachol (sc-202092). Along with cyclosporin A and rapamycin, FK-506 can bind to immunosuppressant binding proteins with high affinity. FK-506 has been found to show neuroregenerative and neuroprotective actions aside from its immunosuppressant activity. Research indicates that FK-506 can stop T cell proliferation in vitro by blocking the generation of a variety of lymphokines, in particular, interleukin (IL-2).
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FK-506 (CAS 104987-11-3) References
- Effect of FK 506 on the cornea: use of topical FK 506 in corneal transplantation in a guinea pig-rat model. | Tchah, H. and Lim, B. 1999. Korean J Ophthalmol. 13: 71-7. PMID: 10761401
- Anti-inflammatory effect of FK-506 on human skin mast cells. | de Paulis, A., et al. 1992. J Invest Dermatol. 99: 723-8. PMID: 1281861
- Neuroregenerative and neuroprotective actions of neuroimmunophilin compounds in traumatic and inflammatory neuropathies. | Gold, BG., et al. 2004. Neurol Res. 26: 371-80. PMID: 15198862
- Chemistry and biology of the immunophilins and their immunosuppressive ligands. | Schreiber, SL. 1991. Science. 251: 283-7. PMID: 1702904
- Monitoring FK 506 concentrations in plasma and whole blood. | Jusko, WJ. and D'Ambrosio, R. 1991. Transplant Proc. 23: 2732-5. PMID: 1721260
- Effect of FK-506 (tacrolimus) therapy on bone healing of titanium implants: a histometric and biomechanical study in mice. | Zheng, X., et al. 2017. Eur J Oral Sci. 125: 28-33. PMID: 27935130
- Therapeutic anti-psoriatic effects of myeloid-derived suppressor cells in combination with systemic tacrolimus (FK-506) in an imiquimod-induced mouse model of psoriasis. | Park, MY., et al. 2020. Int Immunopharmacol. 86: 106553. PMID: 32563057
- Analysis of tacrolimus (FK 506) in relation to therapeutic drug monitoring. | Jusko, WJ. 1995. Ther Drug Monit. 17: 596-601. PMID: 8588227
- Clinical use of FK 506 in liver transplantation. | Klintmalm, GB. 1996. Transplant Proc. 28: 974-6. PMID: 8623484
- Calcineurin mediates calcium-induced potentiation of adenylyl cyclase activity in dispersed chief cells from guinea pig stomach. Further evidence for cross-talk between signal transduction pathways that regulate pepsinogen secretion. | Raufman, JP., et al. 1996. J Biol Chem. 271: 19877-82. PMID: 8702699
- Effects of FK-506 on contraction and Ca2+ transients in rat cardiac myocytes. | McCall, E., et al. 1996. Circ Res. 79: 1110-21. PMID: 8943949
- FK-506 delays corneal graft rejection in a model of corneal xenotransplantation. | Benelli, U., et al. 1996. J Ocul Pharmacol Ther. 12: 425-31. PMID: 8951679
- Mode of action of FK-506 on protective immunity to Hymenolepis nana in mice. | Asano, K., et al. 1996. In Vivo. 10: 537-45. PMID: 8986461
- Neural actions of immunophilin ligands. | Snyder, SH., et al. 1998. Trends Pharmacol Sci. 19: 21-6. PMID: 9509898
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
FK-506, 5 mg | sc-24649 | 5 mg | $76.00 | |||
FK-506, 10 mg | sc-24649A | 10 mg | $148.00 |