FK 506

Name: FK 506
Brand: Tocris Bioscience
SKU: 3631
Rating: 5 (2 reviews)

Catalog # 3631 | Tocris Bioscience a Bio-Techne Brand

(2)

Citations (39)

COA / SDS

Potent calcineurin inhibitor; immunosuppressant

Key Product Details

Description:	Potent calcineurin inhibitor; immunosuppressant
Alternative Names:	Tacrolimus, Fujimycin
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
Purity:	≥99% (HPLC)
Molecular Weight:	804.02

View Full Technical Details for FK 506

Technical Data
Citations (39) / Reviews (2)

Biological Activity for FK 506

FK 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.

Analog also available.

Technical Data for FK 506

M. Wt	804.02
Formula	C₄₄H₆₉NO₁₂
Storage	Store at -20°C
Purity	≥99% (HPLC)
CAS Number	104987-11-3
PubChem ID	445643
InChi Key	QJJXYPPXXYFBGM-LFZNUXCKSA-N
Smiles	O[C@H]1[C@H](OC)C[C@H](/C=C(C)/[C@@H](O4)[C@H](C)[C@@H](O)CC([C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@@]2([H])O[C@](C(C(N3[C@@](C4=O)([H])CCCC3)=O)=O)(O)[C@H](C)C[C@@H]2OC)=O)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for FK 506

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	80.4	100
	ethanol	80.4	100

Preparing Stock Solutions for FK 506

The following data is based on the product molecular weight 804.02.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.24 mL	6.22 mL	12.44 mL
5 mM	0.25 mL	1.24 mL	2.49 mL
10 mM	0.12 mL	0.62 mL	1.24 mL
50 mM	0.02 mL	0.12 mL	0.25 mL

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References for FK 506

References are publications that support the biological activity of the product.

Gordon A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 2020 PMID: 32353859
Sierra-Paredes and Sierra-Marcuno Ascomycin and FK506: Pharmacology and therapeutic potential as anticonvulsants and neuroprotectants. CNS Neurosci.Ther. 2008 PMID: 18482098
Baughman Tissue distribution and abundance of human FKBP51, and FK506-binding protein that can mediate calcineurin inhibition. Biochem.Biophys.Res.Commun. 1997 PMID: 9125197
Fruman 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. 1995 PMID: 7530743

Citations for FK 506 (39)

Showing 1 - 10 of 39 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for FK 506 include:

Hugh P et al. (2023) Dynamic physiological α-synuclein S129 phosphorylation is driven by neuronal activity. NPJ Parkinsons Dis. 9:4
PMID: 36646701
Armando A et al. (2022) Calcineurin Controls Cellular Prion Protein Expression in Mouse Astrocytes. Cells. 11
PMID: 35203261
Kevin et al. (2022) Mild membrane depolarization in neurons induces immediate early gene transcription and acutely subdues responses to a successive stimulus. J Biol Chem. 298:102278
PMID: 35863435
Zhongmei et al. (2022) RASA2 ablation in T cells boosts antigen sensitivity and long-term function. Nature. 609:174-182
PMID: 36002574
Yan et al. (2022) LAMTOR1 inhibition of TRPML1-dependent lysosomal calcium release regulates dendritic lysosome trafficking and hippocampal neuronal function. EMBO J. 41:e108119
PMID: 35099830
Jerzy W et al. (2022) Integrins Bidirectionally Regulate the Efficacy of Inhibitory Synaptic Transmission and Control GABAergic Plasticity. J Neurosci. 42:5830-5842
PMID: 35701161
Satoe et al. (2021) Cell death-inducing cytotoxicity in truncated KCNQ4 variants associated with DFNA2 hearing loss. Dis Model Mech. 14
PMID: 34622280
Paco S et al. (2021) Stepwise disassembly of GABAergic synapses during pathogenic excitotoxicity. Cell Rep. 37:110142
PMID: 34936876
Timothy S et al. (2021) Differential Regulation of ATP- and UTP-Evoked Prostaglandin E2 and IL-6 Production from Human Airway Epithelial Cells. J Immunol. 207:1275-1287
PMID: 34389624
Eleonora et al. (2020) Calcineurin Controls Expression of EAAT1/GLAST in Mouse and Human Cultured Astrocytes through Dynamic Regulation of Protein Synthesis and Degradation. Int J Mol Sci. 21
PMID: 32210081
Douglas et al. (2020) Roles of glycogen synthase kinase 3 alpha and calcineurin in regulating the ability of sperm to fertilize eggs. FASEB J. 34:1247-1269
PMID: 31914663
Mark L et al. (2020) Local miRNA-Dependent Translational Control of GABAAR Synthesis during Inhibitory Long-Term Potentiation. Cell Rep. 31:107785
PMID: 32579917
Christopher J et al. (2020) BCR-Induced Ca2+ Signals Dynamically Tune Survival, Metabolic Reprogramming, and Proliferation of Naive B Cells. Cell Rep. 31:107474
PMID: 32294437
Stuart N et al. (2020) TRESK is a key regulator of nocturnal suprachiasmatic nucleus dynamics and light adaptive responses. Nat Commun. 11:4614
PMID: 32929069
Chiu et al. (2019) NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content. Cell Rep. 28:332
PMID: 31291571
Bradley J et al. (2019) Intracellular Ca2+ Homeostasis and Nuclear Export Mediate Exit from Naive Pluripotency. Cell Stem Cell. 25:210-224.e6
PMID: 31104942
Torres et al. (2018) FK506 Attenuates the MRP1-Mediated Chemoresistant Phenotype in Glioblastoma Stem-Like Cells. Int J Mol Sci. 19
PMID: 30208561
Jing et al. (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol. 1711:351-398
PMID: 29344898
Henson et al. (2017) Long-term depression-associated signaling is required for an in vitro model of NMDA receptor-dependent synapse pruning. Neurobiol Learn Mem. 138:39
PMID: 27794462
Neustadtl et al. (2017) Reduced cortical excitatory synapse number in APOE4 mice is associated with increased calcineurin activity. Neuroreport. 28:618
PMID: 28542068
Stephen R et al. (2017) Calcineurin Dysregulation Underlies Spinal Cord Injury-Induced K+ Channel Dysfunction in DRG Neurons. J Neurosci. 37:8256-8272
PMID: 28751455
Jing et al. (2017) The Effects of Tacrolimus on T-Cell Proliferation Are Short-Lived: A Pilot Analysis of Immune Function Testing. Transplant Direct. 3:e199
PMID: 28795150
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
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
Palmqvist et al. (2016) A human and animal model-based approach to investigating the anti-inflammatory profile and potential of the 5-HT2B receptor antagonist AM1030. J Inflamm (Lond). 13:20
PMID: 27340371
Sharma et al. (2016) Protein Phosphatase 1-α Regulates AS160 Ser588 and Thr642 Dephosphorylation in Skeletal Muscle. Diabetes. 65:2606
PMID: 27246912
Oh et al. (2015) Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons. Iran J Basic Med Sci. 10:162
PMID: 25558061
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
Codeluppi et al. (2014) Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling. PLoS One. 9:e92649
PMID: 24667246
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
Mirante et al. (2014) Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala. J Biol Chem. 7:62
PMID: 25071439
Sharanek et al. (2014) Different dose-dependent mechanisms are involved in early cyclosp. a-induced cholestatic effects in hepaRG cells. Toxicol Sci. 141:244
PMID: 24973091
Lars et al. (2014) Ion channel TRPV1-dependent activation of PTP1B suppresses EGFR-associated intestinal tumorigenesis. J Clin Invest. 124:3793-806
PMID: 25083990
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
Marra et al. (2012) A preferentially segregated recycling vesicle pool of limited size supports neurotransmission in native central synapses. Neuron. 76:579
PMID: 23141069
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
Zhen et al. (2009) Dopamine D4 receptors regulate AMPA receptor trafficking and glutamatergic transmission in GABAergic interneurons of prefrontal cortex. J Neurosci. 29:550-62
PMID: 19144855

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Showing 1 - 10 of 39 citations Showing All

Customer Reviews for FK 506 (2)

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Works as intended.

Name: Anonymous

Species: Rat

Assay Type: In Vitro

Cell Line/Tissue: Sprague-Dawley rats primary neuronal

FK506 for PP2B (FK, 1 μM)

PMID: 31291571 Reference
FK 506, a treatment for primary sclerosing cholangitis

Name: Anonymous

Species: Human

FK 506 was tested for its antibiotic properties. FK 506, a treatment for primary sclerosing cholangitis: results of an open-label preliminary trial.

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