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.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Sierra-Paredes and Sierra-Marcuno (2008) Ascomycin and FK506: Pharmacology and therapeutic potential as anticonvulsants and neuroprotectants. CNS Neurosci.Ther. 14 36. PMID: 18482098.
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.
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.
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Citations are publications that use Tocris products. Selected citations for FK 506 include:
Matsa et al (2016) Transcriptome Profiling of Patient-Specific Human iPSC-Cardiomyocytes Predicts Individual Drug Safety and Efficacy Responses In Vitro. Cell Stem Cell. 19 311. PMID: 27545504 .
Miyamoto et al (2016) Increasing the Receptor Tyrosine Kinase EphB2 Prevents Amyloid-β-induced Depletion of Cell Surface Glutamate Receptors by a Mechanism That Requires the PDZ-binding Motif of EphB2 and Neuronal Activity. Cell Rep 291 1719. PMID: 26589795.
Hadjiasgary et al (2015) Intra-CA1 administration of FK-506 (tacrolimus) in rat impairs learning and memory in an inhibitory avoidance paradigm. J Neurosci 18 130. PMID: 25810886.
Oh et al (2015) Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons. Iran J Basic Med Sci 10 162. PMID: 25558061.
Chiodi et al (2014) Cocaine-induced changes of synaptic transmission in the striatum are modulated by adenosine A2A receptors and involve the tyrosine phosphatase STEP. Neuropsychopharmacology 39 569. PMID: 23989619.
Codeluppi et al (2014) Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling. PLoS One 9 e92649. PMID: 24667246.
Mirante et al (2014) Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala. J Biol Chem 7 62. PMID: 25071439.
Cai et al (2013) Upregulation of nuclear factor of activated T-cells by nerve injury contributes to development of neuropathic pain. J Pharmacol Exp Ther 345 161. PMID: 23386250.
Vliet et al (2013) Human T cell activation results in extracellular signal-regulated kinase (ERK)-calcineurin-dependent exposure of Tn antigen on the cell surface and binding of the macrophage galactose-type lectin (MGL). J Biol Chem 288 27519. PMID: 23918927.
Pont et al (2012) Oxytocin-stimulated NFAT transcriptional activation in human myometrial cells. Mol.Endocrinol. 26 1743. PMID: 22902539.
Lin et al (2011) AKAP79/150 impacts intrinsic excitability of hippocampal neurons through phospho-regulation of A-type K+ channel trafficking. Br J Pharmacol 31 1323. PMID: 21273417.
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Keywords: FK 506, supplier, Potent, calcineurin, inhibitors, inhibits, protein, phosphatases, 2B, Protein, Ser/Thr, FK506, antibiotics, Tocris Bioscience, Protein Ser/Thr Phosphatases Inhibitor products
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