Tacrolimus (FK506)

Catalog No.S5003 Batch:S500313

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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 107 publications

PU.1 and BCL11B sequentially cooperate with RUNX1 to anchor mSWI/SNF to poise the T cell effector landscape [ Nat Immunol, 2024, 25(5):860-872] PubMed: 38632339
Antiviral activity of immunosuppressors alone and in combination against human adenovirus and cytomegalovirus [ Int J Antimicrob Agents, 2024, 63(5):107116] PubMed: 38401774
The mTOR pathway controls phosphorylation of BRAF at T401 [ Cell Commun Signal, 2024, 22(1):428] PubMed: 39223665
Calcineurin inhibitor effects on kidney electrolyte handling and blood pressure: tacrolimus versus voclosporin [ Nephrol Dial Transplant, 2024, gfae119] PubMed: 38777623
FOXO1 promotes cancer cell growth through MDM2-mediated p53 degradation [ J Biol Chem, 2024, 300(4):107209] PubMed: 38519029
Calcineurin-dependent contributions to fitness in the opportunistic pathogen Candida glabrata [ mSphere, 2024, 9(1):e0055423] PubMed: 38171022
(S)-(-)-blebbistatin O-benzoate has the potential to improve atopic dermatitis symptoms in NC/Nga mice by upregulating epidermal barrier function and inhibiting type 2 alarmin cytokine induction [ PLoS One, 2024, 19(5):e0302781] PubMed: 38713650
(S)-(-)-blebbistatin O-benzoate has the potential to improve atopic dermatitis symptoms in NC/Nga mice by upregulating epidermal barrier function and inhibiting type 2 alarmin cytokine induction [ PLoS One, 2024, 19(5):e0302781] PubMed: 38713650
Akap5 links synaptic dysfunction to neuroinflammatory signaling in a mouse model of infantile neuronal ceroid lipofuscinosis [ Front Synaptic Neurosci, 2024, 16:1384625] PubMed: 38798824
Growth patterns of caudal fin rays are informed by both external signals from the regenerating organ and remembered identity autonomous to the local tissue [ bioRxiv, 2024, 2024.03.29.586899] PubMed: 38585773

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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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