Tacrolimus (FK506)

Catalog No.S5003 Batch:S500315

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Technical Data

Formula

C44H69NO12
Molecular Weight 804.02 CAS No. 104987-11-3
Solubility (25°C)* In vitro DMSO 100 mg/mL (124.37 mM)
Ethanol 100 mg/mL (124.37 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Tacrolimus (FK506) is a 23-membered macrolide lactone, it reduces peptidyl-prolyl isomerase activity in T cells by binding to the immunophilin FKBP12 (FK506 binding protein) creating a new complex. Tacrolimus also inhibits the phosphatase activity of calcineurin. Tacrolimus induces vascular endothelial autophagy.
Targets
FKBP12 [1]
(T cells)		 calcineurin [6]
In vitro

FK-506 and cyclosporin A block translocation of the cytoplasmic component without affecting synthesis of the nuclear subunit in T lymphocytes. [1] FK-506 prevents T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. [2] FK 506 binds to distinct families of intracellular proteins (immunophilins) termed cyclophilins and FK 506-binding proteins (FKBPs). FK-506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. [3] FK-506 and CsA exert nearly identical biological effects in cells by inhibiting the same subset of early calcium-associated events involved in lymphokine expression, apoptosis, and degranulation. FK-506 binds to a family of intracellular receptors termed the FK-506 binding proteins (FKBPs). [4]
In vivo

FK-506 results in increase in the paw and tail withdrawal threshold as revealed by behavioral pain assessment in rats against hyperalgesic and allodynic stimuli. FK-506 also leads to a decrease in the serum nitrate and thiobarbituric acid reactive substance (TBARS) levels along with reduction in tissue myeloperoxidase (MPO) and total calcium levels, whereas, rise in tissue reduced glutathione levels in rats. FK-506 ameliorates the increase in the neuronal edema and axonal degeneration in rats with ischemia reperfusion (I/R). [5]

Protocol (from reference)

Cell Assay:

[3]
  • Cell lines

    Jurkat cells

  • Concentrations

    10 nM

  • Incubation Time

    1 h

  • Method

    Cells were cultured in the presence of 10 nM FK 506 for 1 hr and washed, and phosphatase activity was measured in lysates.
Animal Study:

[8]
  • Animal Models

    Male C57BL/6J mice

  • Dosages

    30 mg/kg

  • Administration

    Oral

Customer Product Validation

Data from [Biochim Biophys Acta, 2013, 1833(3), 652-62]

, 2013, Natural and Medical Sciences Institute

, 2013, Natural and Medical Sciences Institute

, 2013, Natural and Medical Sciences Institute

Selleck's Tacrolimus (FK506) has been cited by 94 publications

T cell receptor signaling strength establishes the chemotactic properties of effector CD8+ T cells that control tissue-residency [ Nat Commun, 2023, 14(1):3928] PubMed: 37402742
FKBP12 is a major regulator of ALK2 activity in multiple myeloma cells [ Cell Commun Signal, 2023, 21(1):25] PubMed: 36717825
Calcineurin regulates aldosterone production via dephosphorylation of NFATC4 [ JCI Insight, 2023, 8(14)e157027] PubMed: 37310791
Locally controlled release of immunosuppressive promotes survival of transplanted adult spinal cord tissue [ Regen Biomater, 2023, 10:rbac097] PubMed: 36683735
Calcineurin-mediated dephosphorylation enhances the stability and transactivation of c-Myc [ Sci Rep, 2023, 13(1):13116] PubMed: 37573463
FK506-binding protein 5 regulates cell quiescence-proliferation decision in zebrafish epithelium [ FEBS Lett, 2023, 10.1007/s10565-023-09816-7] PubMed: 37259581
Tacrolimus Maintains the Balance of Neutrophil Extracellular Traps by Inducing DNA Methylation of Neutrophils to Reduce Immune Rejection [ Life (Basel), 2023, 13(12)2253] PubMed: 38137854
Antagonistic effect of cyclin-dependent kinases and a calcium-dependent phosphatase on polyglutamine-expanded androgen receptor toxic gain of function [ Sci Adv, 2023, 9(1):eade1694] PubMed: 36608116
Immunosuppression with Cyclosporine versus Tacrolimus shows distinctive nephrotoxicity profiles within renal compartments [ bioRxiv, 2023, 10.1101/2023.04.05.535688 ] PubMed: none
The role of IL-18 and IL-1 receptor signaling in T cell development and T cell exhaustion in a murine pancreatic cancer model [ Philipps-Universität Marburg, 2023, 10.17192/z2023.0576] PubMed: none

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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