Cat. No. 3631
Alternative Names: Tacrolimus, Fujimycin
Chemical Name: (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R
Biological ActivityPotent 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 (IC50 = 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.
Certificate of Analysis / Safety Data Sheet
Fruman et al (1995) 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. J.Immunol. 154 1846. PMID: 7530743.
Baughman et al (1997) Tissue distribution and abundance of human FKBP51, and FK506-binding protein that can mediate calcineurin inhibition. Biochem.Biophys.Res.Commun. 232 437. PMID: 9125197.
Sierra-Paredes and Sierra-Marcuno (2008) Ascomycin and FK506: Pharmacology and therapeutic potential as anticonvulsants and neuroprotectants. CNS Neurosci.Ther. 14 36. PMID: 18482098.
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Keywords: FK 506, supplier, Potent, calcineurin, inhibitors, protein, phosphatases, 2B, Protein, Ser/Thr, FK506, antibiotics
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