Potent calcineurin (protein phosphatase 2B) inhibitor that requires FK 506-binding protein 12 (FKBP12) for activity (IC50
= 3 nM). Inhibits secretion of IL-1, IL-2 (IC50
= 1 nM), IL-3, IL-4, IL-6 (IC50
= 35 nM), GM-CSF, TNFα
= 10 nM), IFNγ
and Myc from activated T cells in vitro
. Exhibits potent immunosuppressive, neuroprotective and anticonvulsant activity in vivo
. Analog (ascomycin
, Cat. No. 4210) also available.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Other Product-Specific Information:
The complex of FK506-binding protein 12 and FK506 inhibits calcineurin phosphatase activity and IgE activation-induced cytokine transcripts, but not exocytosis, in mouse mast cells.
Fruman et al.
Tissue distribution and abundance of human FKBP51, and FK506-binding protein that can mediate calcineurin inhibition.
Baughman et al.
Ascomycin and FK506: Pharmacology and therapeutic potential as anticonvulsants and neuroprotectants.
Sierra-Paredes and Sierra-Marcuno
CNS Neurosci.Ther., 2008;14:36
The citations listed below are publications that use Tocris products. Selected citations for FK 506 include:
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