Structure of FK-506
Dose response inhibition of IL-2 secretion by FK-506 in Jurkat cells treated overnight with TPA (40 nM) and A23187 (2 μM).
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.
Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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).
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