Home / Protein Ser/Thr Phosphatase Inhibitors / FK 506

FK 506

Catalog #: 3631
39 Citations Datasheet
Catalog # Availability Size / Price Qty
3631/10
FK 506 | CAS No. 104987-11-3 | Protein Ser/Thr Phosphatase Inhibitors
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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%

Product Details
Citations (39)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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

M.Wt:
804.02
Formula:
C44H69NO12
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥99%
Storage:
Store at -20°C
CAS No:
104987-11-3

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.

Additional Information

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Citations for FK 506

The citations listed below are publications that use Tocris products. Selected citations for FK 506 include:

39 Citations: Showing 1 - 10

  1. Dynamic physiological α-synuclein S129 phosphorylation is driven by neuronal activity.
    Authors: Hugh P Et al.
    NPJ Parkinsons Dis  2023;9:4
  2. RASA2 ablation in T cells boosts antigen sensitivity and long-term function.
    Authors: Zhongmei Et al.
    Nature  2022;609:174-182
  3. Integrins Bidirectionally Regulate the Efficacy of Inhibitory Synaptic Transmission and Control GABAergic Plasticity.
    Authors: Jerzy W Et al.
    J Neurosci  2022;42:5830-5842
  4. LAMTOR1 inhibition of TRPML1-dependent lysosomal calcium release regulates dendritic lysosome trafficking and hippocampal neuronal function.
    Authors: Yan Et al.
    EMBO J  2022;41:e108119
  5. Mild membrane depolarization in neurons induces immediate early gene transcription and acutely subdues responses to a successive stimulus.
    Authors: Kevin Et al.
    J Biol Chem  2022;298:102278
  6. Calcineurin Controls Cellular Prion Protein Expression in Mouse Astrocytes.
    Authors: Armando A Et al.
    Cells  2022;11
  7. Stepwise disassembly of GABAergic synapses during pathogenic excitotoxicity.
    Authors: Paco S Et al.
    Cell Rep  2021;37:110142
  8. Differential Regulation of ATP- and UTP-Evoked Prostaglandin E2 and IL-6 Production from Human Airway Epithelial Cells.
    Authors: Timothy S Et al.
    J Immunol  2021;207:1275-1287
  9. Cell death-inducing cytotoxicity in truncated KCNQ4 variants associated with DFNA2 hearing loss.
    Authors: Satoe Et al.
    Dis Model Mech  2021;14
  10. Roles of glycogen synthase kinase 3 alpha and calcineurin in regulating the ability of sperm to fertilize eggs.
    Authors: Douglas Et al.
    FASEB J  2020;34:1247-1269
  11. Local miRNA-Dependent Translational Control of GABAAR Synthesis during Inhibitory Long-Term Potentiation.
    Authors: Mark L Et al.
    Cell Rep  2020;31:107785
  12. BCR-Induced Ca2+ Signals Dynamically Tune Survival, Metabolic Reprogramming, and Proliferation of Naive B Cells.
    Authors: Christopher J Et al.
    Cell Rep  2020;31:107474
  13. Calcineurin Controls Expression of EAAT1/GLAST in Mouse and Human Cultured Astrocytes through Dynamic Regulation of Protein Synthesis and Degradation.
    Authors: Eleonora Et al.
    Int J Mol Sci  2020;21
  14. TRESK is a key regulator of nocturnal suprachiasmatic nucleus dynamics and light adaptive responses.
    Authors: Stuart N Et al.
    Nat Commun  2020;11:4614
  15. NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
    Authors: Chiu Et al.
    Cell Rep  2019;28:332
  16. Intracellular Ca2+ Homeostasis and Nuclear Export Mediate Exit from Naive Pluripotency.
    Authors: Bradley J Et al.
    Cell Stem Cell  2019;25:210-224.e6
  17. FK506 Attenuates the MRP1-Mediated Chemoresistant Phenotype in Glioblastoma Stem-Like Cells.
    Authors: Torres Et al.
    Int J Mol Sci  2018;19
  18. Methods for High-throughput Drug Combination Screening and Synergy Scoring.
    Authors: Jing Et al.
    Methods Mol Biol  2018;1711:351-398
  19. The Effects of Tacrolimus on T-Cell Proliferation Are Short-Lived: A Pilot Analysis of Immune Function Testing.
    Authors: Jing Et al.
    Transplant Direct  2017;3:e199
  20. Calcineurin Dysregulation Underlies Spinal Cord Injury-Induced K+ Channel Dysfunction in DRG Neurons.
    Authors: Stephen R Et al.
    J Neurosci  2017;37:8256-8272
  21. Reduced cortical excitatory synapse number in APOE4 mice is associated with increased calcineurin activity.
    Authors: Neustadtl Et al.
    Neuroreport  2017;28:618
  22. 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
  23. Protein Phosphatase 1-α Regulates AS160 Ser588 and Thr642 Dephosphorylation in Skeletal Muscle.
    Authors: Sharma Et al.
    Diabetes  2016;65:2606
  24. 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
  25. 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
  26. 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
  27. 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
  28. Heterosynaptic structural plasticity on local dendritic segments of hippocampal CA1 neurons.
    Authors: Oh Et al.
    Iran J Basic Med Sci  2015;10:162
  29. Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling.
    Authors: Codeluppi Et al.
    PLoS One  2014;9:e92649
  30. Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala.
    Authors: Mirante Et al.
    J Biol Chem  2014;7:62
  31. 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.
    Neuropsychopharmacology  2014;39:569
  32. 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
  33. Ion channel TRPV1-dependent activation of PTP1B suppresses EGFR-associated intestinal tumorigenesis.
    Authors: Lars Et al.
    J Clin Invest  2014;124:3793-806
  34. 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
  35. 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
  36. A preferentially segregated recycling vesicle pool of limited size supports neurotransmission in native central synapses.
    Authors: Marra Et al.
    Neuron  2012;76:579
  37. Oxytocin-stimulated NFAT transcriptional activation in human myometrial cells.
    Authors: Pont Et al.
    Mol.Endocrinol.  2012;26:1743
  38. 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
  39. Dopamine D4 receptors regulate AMPA receptor trafficking and glutamatergic transmission in GABAergic interneurons of prefrontal cortex.
    Authors: Zhen Et al.
    J Neurosci  2009;29:550-62

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