Tacrolimus (FK506)

Catalog No.S5003 Synonyms: FR900506

Tacrolimus (FK506) Chemical Structure

Molecular Weight(MW): 804.02

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.

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In DMSO USD 140 In stock
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USD 170 In stock
USD 430 In stock
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Cited by 16 Publications

7 Customer Reviews

  • Effect of FK506 on cytosolic calcium homeostasis induced by TG and thrombin in human platelets. (A-B) Human platelets were suspended in a Ca 2+-free medium (100 µM of EGTA was added as indicated by arrowhead), and preincubated for 5 min at 37oC in the absence (solid black traces) or presence of increased concentrations (0.01-100 µM) of FK506 (light-doted and dark solid-grey traces, respectively). Cells were then stimulated with TG (200 nM; A) or Thr (0.1 U/mL; B) and 3 min later 300 μM of CaCl2 was added to extracellular medium to visualize calcium entry.

    Biochim Biophys Acta 2013 1833(3), 652-62. Tacrolimus (FK506) purchased from Selleck.

  • Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. I IL-17A, J TARC, K IL-13, L IL-1ra, M IL-5, N IL-10.

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

  • Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. A IL-1β, B IL-6, C IFNγ, D MCP-1

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

  • Release of immune mediators after Tacrolimus application. Tacrolimus was applied to IL-1β/TNFα pretreated (diamonds) or unprimed (squares) Caco-2 monolayer in the indicated concentrations. Caco-2 cells in transwell inserts were transferred to culture vessels filled with heparinized whole blood of three different healthy donors (indicated by their ID-numbers). After 1 h the whole blood in the lower compartment was stimulated by LPS/SEB/anti-CD28 injection. After 6 h the Caco-2 cells were removed and the whole blood was further incubated for 18 h. Immune mediators were quantified in plasma. Depicted are stimulation indices of single experiments. E IL-8, F IP-10, G TNFα, H IL-4

    2013 Natural and Medical Sciences Institute. Tacrolimus (FK506) purchased from Selleck.

  • FK506 reduces NCCE(Non-capacitative calcium entry) independently of its inhibitory effect in CaN activity. Fura-2-loaded human platelets were suspended in HBS medium containing 300 μM Ca2+ and preincubated for 5 min with increasing concentration of FK506 (0.5-50 μM), after which OAG (100 μM) was added to initiate NCCE.

    Biochim Biophys Acta, 2015, 1853(10 Pt A):2684-96.. Tacrolimus (FK506) purchased from Selleck.

  • FK506 production of S. tsukubaensis L19 and its recombinant pression of fkbN in S. tsukubaensis L19); L22, S. tsukubaensis L22 (overexpression of tcs7 in S. tsukubaensis L19); L23, S. tsukubaensis L23 (overexpression of fkbN and tcs7 in S. tsukubaensis L19).

    J Ind Microbiol Biotechnol, 2016, 43(12):1693-1703.. Tacrolimus (FK506) purchased from Selleck.

  • JCI Insight, 2016, 1(10):e86331.. Tacrolimus (FK506) purchased from Selleck.

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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.
Targets
FKBP12 [1]
(T cells)
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
rat RBL2H3 cells MXrGeY5kfGmxbjDhd5NigQ>? M2D5TFE3KGh? M1Gy[mlvcGmkaYTpc44hd2ZiVF7GMYFteGijIIDyc4R2[3Srb36gbY4hemG2IGLCUFJJOyClZXzsd{Bi\nSncjCxOkBpenNiYomgSWxKW0FuIFnDOVA:OC5{NTDuUS=> M3X1TVI{PzlzMEe2
rat RBL2H3 cells Mo\vSpVv[3Srb36gZZN{[Xl? M{nnWFE2KG2rboO= NF;SXZVCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKHKjdDDSRmwzUDNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBFVlBvQmPBMYlv\HWlZXSgWG5HNWGucHjhJJBzd2S3Y4Tpc44heHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJJBzcW:{IFTOVE1DW0FiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliRVzJV2EtKEmFNUC9NE4zPSCwTR?= NVHaWIVMOjJ2MUCwPFQ>
human T-cell NXXT[odVWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWfhT2JiUW5idnn0do8hcW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJHQu[2WubDDwdo9tcW[ncnH0bY9vNCCLQ{WwQVAvPSCwTR?= MVK3OVM4OzNz
human WiDr cells MkjaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoDsTY5pcWKrdHnvckBw\iCVQWCxN|AhdWWmaXH0[YQh[2WubDDndo94fGhiaX6gbJVu[W5iV3nEdkBk\WyuczygTWM2OD1zMD65JI5O NV7Re|l1OTd4NEOxNVI>
human U251 cells NXrNbXg1TnWwY4Tpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKFODUEGzNEBqdiCYRVfGMZN1cW23bHH0[YQhcHWvYX6gWVI2OSClZXzsd{BjgSCSTFHQJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NVMvQCCwTR?= NEXH[YoyPzZ2M{GxNi=>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin; 

PubMed: 26455952     


Representative immunoblots and quantitative analysis of synaptosomes from cultured mutant hippocampal neurons in the presence and absence of FK506 treatment showing a selective increase in total GluA1 and GluA1 S845 phosphorylation [pGluA1(S845)] (n=10 experiments, *p<0.05 and ***p<0.001, unpaired two-tailed student's t-test). 

p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3; 

PubMed: 23470533     


Effect of FK506 on protein expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3. Cells were incubated either in the absence of (control) or in the presence of FK506 (12.5, 25 and 50 μM) for 8 h, and protein expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3 were determined using western blotting. Increasing expressions of p-JNK, p-ERK, cytosolic cytochrome c and cleaved caspase-3 were observed in fibroblasts after FK506 treatment at increasing concentrations, and peaked at the concentration of 50 μM.

p-S6K(S371) / S6K / p-Erα(S167) / Erα; 

PubMed: 29344249     


MCF-7 cells were incubated with PS, OA (100 nM), Cal A (1 nM), FK506 (10 nM), or DMSO (0.1%, vehicle) in E2 (10 nM) medium. Phosphorylation was determined by western blotting. 

26455952 23470533 29344249
Immunofluorescence
FKBP52 / p23 / hsp90; 

PubMed: 20796173     


Subcellular localization of FKBP52, hsp90 and p23 in N2a cells. (a) Images by confocal microscopy of undifferentiated cells prior (0 h) or after (3 h and 24 h) of treatment with FK506. Image on the right hand shows a wider field.

FKBP51; 

PubMed: 20796173     


FKBP51 concentrates in transcriptionally active nuclear domains. Cells were treated with FK506 for 6 h and pre-mRNAs were labeled with Br-UTP. Bars= 10 μm

Tom20 / JC-1 / ROS / NF-κB; 

PubMed: 30294901     


TH2849 protects mitochondrial from damage induced by MPP+. Representative confocal image of MDA‐MB‐231 cells incubated with treated with 1‰ DMSO, 10 μmol/L MPP+ alone, or co‐treated with 1 μmol/L rapamycin, 10 μmol/L FK506, 1 μmol/L TH 2451, and 1 μmol/L TH 2849 for 24 h, and then, the immunofluorescence experiment was performed with the primary antibody against (A) Tom20 and (D) NF‐Κb, or the fluorogenic probe DCFH‑DA was used to detect the ROS levels (C). B, EGFP‐LC3 transfected PC12 cells were treated with 10 μmol/L MPP+ alone or co‐treated with 1‰ DMSO, 1 μmol/L rapamycin, 10 μmol/L FK506, 1 μmol/L TH 2451, and 1 μmol/L TH 2849 for 24 h. Mitochondrial transmembrane potential (ΔΨm) was detected by JC‐1. All the substances were dissolved in DMSO. Scale bars: 10 μm. n = 3

20796173 30294901
Growth inhibition assay
Cell viability; 

PubMed: 23470533     


Effect of FK506 on fibroblast proliferation in vitro. Rat skin fibroblasts were treated with increasing concentrations of FK506 for 8 h. The viable cells were measured by CCK-8 assay. FK506 inhibited fibroblast proliferation in a dose-dependent manner. Cell viability reached a relatively minimal level at 75 μM. *P<0.05, **P<0.01 compared with control. All experiments were preformed three times with comparable results

23470533
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

Solubility (25°C)

In vitro DMSO 94 mg/mL (116.91 mM)
Ethanol 83 mg/mL (103.23 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing. 		15mg/mL

* 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.

Chemical Information

Molecular Weight 804.02
Formula

C44H69NO12
CAS No. 104987-11-3
Storage powder
in solvent
Synonyms FR900506

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04078750 Not yet recruiting Behavioral: Tailored medication adherence plan Kidney Disease Chronic|Medication Adherence|Renal Disease|Kidney Rejection Transplant University of British Columbia September 2019 Not Applicable
NCT04045171 Not yet recruiting Drug: Tacrolimus Nephrotic Syndrome|Tacrolimus|Pharmacokinetics The Third Xiangya Hospital of Central South University|Hunan Provincial People''s Hospital|ZhuZhou Central Hospital|First People''s Hospital of Chenzhou August 10 2019 --
NCT03979365 Not yet recruiting Drug: Envarsus XR|Drug: Tacrolimus twice daily Kidney Transplant Recipients Mayo Clinic|Veloxis Pharmaceuticals July 1 2019 Phase 4
NCT04023760 Recruiting Drug: Apixaban Pharmacokinetics|Kidney Transplant|Lung Transplant University of Saskatchewan|Saskatchewan Health Research Foundation|Lung Association of Saskatchewan June 26 2019 Phase 4

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    we would like to inject it subcutaneously into rats, Can we mix the FK506 with 5% dextrose to a concentration of 5mg/ml to prepare the solution?

  • Answer:

    You can dissolve FK506 with DMSO to prepare the stock solution, and then dilute by 5% dextrose. However, we don't have the information about the solubility in this condiation. Or you can use the vehicle we tested: 30% PEG400/0.5% Tween80/5% propylene glycol (Solubility: 30mg/ml).

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID