Chemical Name: (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propen-1-yl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)tetrone
Biological ActivityFK 506 is a 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 (IC50 = 10 nM), IFNγ and Myc from activated T cells in vitro. Exhibits potent immunosuppressive, neuroprotective and anticonvulsant activity in vivo. Identified as targeting human host cell proteins that interact with SARS-CoV-2.
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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
A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing.
Gordon et al.
Citations for FK 506
The citations listed below are publications that use Tocris products. Selected citations for FK 506 include:
19 Citations: Showing 1 - 10
NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
Authors: Chiu Et al.
Cell Rep 2019;28:332
FK506 Attenuates the MRP1-Mediated Chemoresistant Phenotype in Glioblastoma Stem-Like Cells.
Authors: Torres Et al.
Int J Mol Sci 2018;19
Reduced cortical excitatory synapse number in APOE4 mice is associated with increased calcineurin activity.
Authors: Neustadtl Et al.
Long-term depression-associated signaling is required for an in vitro model of NMDA receptor-dependent synapse pruning.
Authors: Henson Et al.
Neurobiol Learn Mem 2017;138:39
Protein Phosphatase 1-α Regulates AS160 Ser588 and Thr642 Dephosphorylation in Skeletal Muscle.
Authors: Sharma Et al.
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.
Authors: Miyamoto Et al.
Cell Rep 2016;291:1719
Transcriptome Profiling of Patient-Specific Human iPSC-Cardiomyocytes Predicts Individual Drug Safety and Efficacy Responses In Vitro.
Authors: Matsa Et al.
Cell Stem Cell. 2016;19:311
A human and animal model-based approach to investigating the anti-inflammatory profile and potential of the 5-HT2B receptor antagonist AM1030.
Authors: Palmqvist Et al.
J Inflamm (Lond) 2016;13:20
Intra-CA1 administration of FK-506 (tacrolimus) in rat impairs learning and memory in an inhibitory avoidance paradigm.
Authors: Hadjiasgary Et al.
J Neurosci 2015;18:130
Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons.
Authors: Oh Et al.
Iran J Basic Med Sci 2015;10:162
Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling.
Authors: Codeluppi Et al.
PLoS One 2014;9:e92649
Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala.
Authors: Mirante Et al.
J Biol Chem 2014;7:62
Cocaine-induced changes of synaptic transmission in the striatum are modulated by adenosine A2A receptors and involve the tyrosine phosphatase STEP.
Authors: Chiodi Et al.
Different dose-dependent mechanisms are involved in early cyclosp. a-induced cholestatic effects in hepaRG cells.
Authors: Sharanek Et al.
Toxicol Sci 2014;141:244
Upregulation of nuclear factor of activated T-cells by nerve injury contributes to development of neuropathic pain.
Authors: Cai Et al.
J Pharmacol Exp Ther 2013;345:161
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).
Authors: Vliet Et al.
J Biol Chem 2013;288:27519
A preferentially segregated recycling vesicle pool of limited size supports neurotransmission in native central synapses.
Authors: Marra Et al.
Oxytocin-stimulated NFAT transcriptional activation in human myometrial cells.
Authors: Pont Et al.
AKAP79/150 impacts intrinsic excitability of hippocampal neurons through phospho-regulation of A-type K+ channel trafficking.
Authors: Lin Et al.
Br J Pharmacol 2011;31:1323
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FK 506 was tested for its antibiotic properties. FK 506, a treatment for primary sclerosing cholangitis: results of an open-label preliminary trial.