Tacrolimus (FK506)

For research use only.

Catalog No.S5003 Synonyms: FR900506, Fujimycin, Prograf

55 publications

Tacrolimus (FK506) Chemical Structure

CAS No. 104987-11-3

Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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.

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Selleck's Tacrolimus (FK506) has been cited by 55 publications

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Biological Activity

Description Tacrolimus (FK506, FR900506, Fujimycin, Prograf) 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U251 cells NETpelZHfW6ldHnvckBie3OjeR?= MXLJcohq[mm2aX;uJI9nKFODUEGzNEBqdiCYRVfGMZN1cW23bHH0[YQhcHWvYX6gWVI2OSClZXzsd{BjgSCSTFHQJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9NVMvQCCwTR?= NFnvNXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[0N|EyOid-MUe2OFMyOTJ:L3G+
human WiDr cells NEDodJlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX\sbnRpUW6qaXLpeIlwdiCxZjDTRXAyOzBibXXkbYF1\WRiY3XscEBoem:5dHigbY4hcHWvYX6gW4lFeiClZXzsd{whUUN3ME2xNE46KG6P MknaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd4NEOxNVIoRjF5NkSzNVEzRC:jPh?=
human T-cell MUnQdo9tcW[ncnH0bY9vKGG|c3H5 M3LITWlvKH[rdILvJIlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUMYNmdGxicILvcIln\XKjdHnvckwhUUN3ME2wMlUhdk1? NInrfWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi95NUO3N|MyLz55NUO3N|MyRC:jPh?=
rat RBL2H3 cells NW\iRXpxTnWwY4Tpc44h[XO|YYm= NIHVSnMyPSCvaX7z MW\BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJJJifCCUQlyyTFMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDEUnAuSlODLXnu[JVk\WRiVF7GMYFteGijIIDyc4R2[3Srb36gdJJmcW6ldXLheIVlKG[xcjCxOUBucW6|IIDybY9zKESQUD3CV2Eh[2ijbHzlcodmKG2nYYP1doVlKGGodHXyJFMxKG2rboOgZpkhTUyLU1GsJGlEPTB;MD6yOUBvVQ>? M2LiVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEGwNFg1Lz5{MkSxNFA5PDxxYU6=
rat RBL2H3 cells NXr2eFU4TnWwY4Tpc44h[XO|YYm= NUP1fJRqOTZiaB?= M{HhT2lvcGmkaYTpc44hd2ZiVF7GMYFteGijIIDyc4R2[3Srb36gbY4hemG2IGLCUFJJOyClZXzsd{Bi\nSncjCxOkBpenNiYomgSWxKW0FuIFnDOVA:OC5{NTDuUS=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MUC3Okc,OjN5OUGwO|Y9N2F-
PBMCs MmnRSpVv[3Srb36gZZN{[Xl? NHX4SZNKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUU[QLXfhcY1iKHC{b3T1Z5Rqd25iKFHueIkuS0R|IH3vco9kdG:wYXygZY51cWKxZImgd5RqdXWuYYTl[EBidmRiY4XseJVz\WRiQ1S0JJBwe2m2aY\lJINmdGy|IID1dolncWWmIH\yc40hcHWvYX6gdIVzcXCqZYLhcEBjdG:xZDDtc45wdnWlbHXhdkBk\WyuKTygTWM2OCB;IECuNFAxODZizszNMi=> NIj1eVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUO2PVM6QSd-MUWzOlk{QTl:L3G+
PBMCs MUnGeY5kfGmxbjDhd5NigQ>? M1rZT2lvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBKVC13IIDyc4R2[3Srb36gLGFvfGlvQ1SzJI1wdm:lbH;uZYwh[W62aXLv[Jkhe3SrbYXsZZRm\CCjbnSgZ5VtfHW{ZXSgR2Q1KHCxc3n0bZZmKGOnbHzzJJB2emmoaXXkJIZzd21iaIXtZY4heGW{aYDo[ZJidCCkbH;v[EBud26xboXjcIVieiClZXzsLUwhUUN3MDC9JFAvODByME[g{txONg>? M{LI[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{[5N|k6Lz5zNUO2PVM6QTxxYU6=
T-cells NUnxTGYxTnWwY4Tpc44h[XO|YYm= Ml73WIhmKGOxbYDveY5lKHejczD0[ZN1\WRiZn;yJIl1eyCrbnjpZol1d3K7IHHjeIl3cXS7IHHnZYlve3RiVD3j[YxtKHC{b3zp[oVz[XSrb36geZNqdmdibYXybY5mKHOybHXubYMhXC2lZXzsd{whUUN3MDC9JFAvODByMjFOwG0v NWjUeIl{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUC0OVA6QDdpPkGwOFUxQTh5PD;hQi=>
RBL-2H3 MYPGeY5kfGmxbjDhd5NigQ>? MkLXTY5pcWKrdHnvckBw\iCGTmC3MWJUSSCjboTp[4VvNWmwZIXj[YQhXE6IYXzwbIEhemWuZXHz[UBqdiC{YYSgVmJNNTKKMzDj[YxteyxiSVO1NEA:KDBwMECwNlUh|ryPLh?= MnTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ7MEG2PVYoRjF4OUCxOlk3RC:jPh?=
Jurkat T M1n5UmludXWwb4P1dJBz\XO|aY\lJIF{e2G7 M4\meVE2KHSxIEOwJI1qdnN? NVW2U2lPUW2vdX7vd5VxeHKnc4PpeoUh[WO2aY\peJkhcW5iUF3BM4lwdm:veXPpckB{fGmvdXzheIVlKGi3bXHuJGp2emujdDDUJINmdGy|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIFnMNkBxem:mdXP0bY9vKHC{ZYTy[YF1\WRiZn;yJFE2KHSxIEOwJI1qdnNiZn;scI94\WRiYomgVG1CN2mxbn;tfYNqdiCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAyQCC2bzCyNEBpenNiYomgSWxKW0FuIFnDOVAhRSByLkO2JO69VS5? MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDRzMkKwOEc,Ojh2MUKyNFQ9N2F-
HEK293 M3LTZ2Z2dmO2aX;uJIF{e2G7 NEHwOlNVWF:WUlHOV3BQWlSHUkqgbY5pcWKrdHnvckBw\iCSaHHscI9q\GmwIIXweIFs\SBqUHjhcIxwcWSrbkqgNUB2VSliaX6gU2FVWC2FLXX4dJJme3OrbnegTGVMOjl|IHPlcIx{NCCLQ{WwJF0hOy55IN88UU4> NELnPG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNEWzNFkxPyd-MUS1N|A6ODd:L3G+
Jurkat T NVPqd|NOSW62aXnu[oxidW2jdH;yfUBie3OjeR?= NHnvbVMzOCCvaX7z Ml7QRY51cS2rbn\sZY1u[XSxcomgZYN1cX[rdImgbY4hWE2DL3nvco9ugWOrbjDzeIlufWyjdHXkJIh2dWGwIFr1dotifCCWIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBKVC1{IIPlZ5JmfGmxbjDwdoVqdmO3YnH0[YQh\m:{IEKwJI1qdnNiZn;scI94\WRiYomgVG1CN2mxbn;tfYNqdiC|dHnteYxifGmxbjDt[YF{fXKnZDDh[pRmeiBzMjDodpMh[nliRVzJV2EtKEmFNUCgQUA2NjhizszNMi=> MmDaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3MEm1OVIoRjJ6NUC5OVUzRC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
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. 

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.

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). 

29344249 23470533 26455952
Immunofluorescence
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

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

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.

30294901 20796173
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, Fujimycin, Prograf
Smiles CC1CC(C2C(CC(C(O2)(C(=O)C(=O)N3CCCCC3C(=O)OC(C(C(CC(=O)C(C=C(C1)C)CC=C)O)C)C(=CC4CCC(C(C4)OC)O)C)O)C)OC)OC

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04645667 Recruiting Drug: Tacrolimus Acute GVHD UNC Lineberger Comprehensive Cancer Center|University of North Carolina Chapel Hill February 1 2021 --
NCT04720326 Recruiting Drug: Tacrolimus Pill|Drug: Tacrolimus capsule Prophylaxis Against Liver Transplant Rejection Edward Geissler|Chiesi GmbH|Excelya Germany GmbH|University of Regensburg December 23 2020 Phase 4
NCT04646356 Recruiting Drug: Tacrolimus capsule (low-dose)|Drug: Placebo Hereditary Hemorrhagic Telangiectasia|Epistaxis Nosebleed Unity Health Toronto|United States Department of Defense October 20 2020 Phase 2
NCT04633733 Active not recruiting Drug: HL237 tablet|Drug: tacrolimus capsule Healthy Male Volunteers Hanlim Pharm. Co. Ltd. August 22 2020 Phase 1

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