Tacrolimus (FK506)

For research use only.

Catalog No.S5003 Synonyms: FR900506

28 publications

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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10mM (1mL in DMSO) USD 140 In stock
USD 90 In stock
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Selleck's Tacrolimus (FK506) has been cited by 28 publications

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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.
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 NVPsUI1mTnWwY4Tpc44h[XO|YYm= NHzJZZMyPiCq M{fRU2lvcGmkaYTpc44hd2ZiVF7GMYFteGijIIDyc4R2[3Srb36gbY4hemG2IGLCUFJJOyClZXzsd{Bi\nSncjCxOkBpenNiYomgSWxKW0FuIFnDOVA:OC5{NTDuUS=> NFHy[4szOzd7MUC3Oi=>
rat RBL2H3 cells NWfoWm9{TnWwY4Tpc44h[XO|YYm= NYL0bnhFOTVibXnudy=> NFPs[oNCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKHKjdDDSRmwzUDNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBFVlBvQmPBMYlv\HWlZXSgWG5HNWGucHjhJJBzd2S3Y4Tpc44heHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJJBzcW:{IFTOVE1DW0FiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliRVzJV2EtKEmFNUC9NE4zPSCwTR?= MmryNlI1OTByOES=
human T-cell NVfhV3FCWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4O1ZmlvKH[rdILvJIlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUMYNmdGxicILvcIln\XKjdHnvckwhUUN3ME2wMlUhdk1? NIG5ZZk4PTN5M{Ox
human WiDr cells Mmm3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVvNRlRMUW6qaXLpeIlwdiCxZjDTRXAyOzBibXXkbYF1\WRiY3XscEBoem:5dHigbY4hcHWvYX6gW4lFeiClZXzsd{whUUN3ME2xNE46KG6P NWXLPIVGOTd4NEOxNVI>
human U251 cells M1vXc2Z2dmO2aX;uJIF{e2G7 Mn3mTY5pcWKrdHnvckBw\iCVQWCxN|AhcW5iVlXHSk1{fGmvdXzheIVlKGi3bXHuJHUzPTFiY3XscJMh[nliUFzBVEBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwQVE{Njhibl2= MUSxO|Y1OzFzMh?=

... Click to View More Cell Line Experimental Data

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
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.


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

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]


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.

* 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


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
NCT03910868 Not yet recruiting -- Liver Transplantation|Kidney Transplantation Rennes University Hospital June 2020 --
NCT04292418 Not yet recruiting Drug: Tacrolimus capsule mycophenolic acid Rejection Acute Renal Assiut University May 1 2020 --
NCT04341038 Recruiting Drug: Tacrolimus|Drug: Methylprednisolone COVID-19|Lung Injury Hospital Universitari de Bellvitge|Institut d''Investigació Biomèdica de Bellvitge April 1 2020 Phase 3
NCT04360031 Recruiting Drug: Tacrolimus Kidney Transplant; Complications|Immunosuppression|Transplant Failure Université Catholique de Louvain February 10 2020 --

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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