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10007965 FK-506
Tacrolimus
(CAS 104987-11-3)
FK-506 Workbook Links
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FK-506 is a potent, clinically-useful immunosuppressant in the same molecular class as cyclosporin A and rapamycin.1 Its mechanism of action involves the formation of a high affinity complex (Ki = 0.2 nM) with FK-506 Binding Protein 12 (FKBP12). This complex then inhibits the activity of the calcium/calmodulin-dependent protein phosphatase, calcineurin, leading to disruption of T-cell activation.2 The physiological effects of FK-506 also include regulation of nitric oxide neurotoxicity, neurotransmitter release, and regulation of Ca2+ release via the ryanodine and inositol-(1,4,5)-trisphosphate (IP3) receptors.3 In the latter case, FKBP12 forms a tight complex with both ryanodine and IP3 receptors which can be disrupted by FK-506, thereby rendering the receptors “leaky” to Ca2+.
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1
Schreiber, S.L. Chemistry and biology of the immunophilins and their immunosuppressive ligands. Science 251 283-287 (1991).
2
Dumont, F.J. FK506, An immunosuppressant targeting calcineurin function. Current Medicinal Chemistry 7 731-748 (2000).
3
Snyder, S.H., Sabatini, D.M., Lai, M.M., et al. Neural actions of immunophilin ligands. tips 19 21-26 (1998).
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Pricing updated 2010-03-19.
Prices are subject to change without notice.
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