Tacrolimus (FK506)

Catalog No.S5003 Synonyms: FR900506, Fujimycin, Prograf

For research use only.

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.

Tacrolimus (FK506) Chemical Structure

CAS No. 104987-11-3

Selleck's Tacrolimus (FK506) has been cited by 65 publications

Purity & Quality Control

Choose Selective FKBP Inhibitors

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 MXXGeY5kfGmxbjDhd5NigQ>? NGTqc2ZKdmirYnn0bY9vKG:oIGPBVFE{OCCrbjDWSWdHNXO2aX31cIF1\WRiaIXtZY4hXTJ3MTDj[YxteyCkeTDQUGFRKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:OTNwODDuUS=> MlPUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd4NEOxNVIoRjF5NkSzNVEzRC:jPh?=
human WiDr cells NIDoUFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4XRRWlvcGmkaYTpc44hd2ZiU1HQNVMxKG2nZHnheIVlKGOnbHyg[5Jwf3SqIHnuJIh2dWGwIGfpSJIh[2WubIOsJGlEPTB;MUCuPUBvVQ>? M3XtfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NkSzNVEzLz5zN{[0N|EyOjxxYU6=
human T-cell M4qw[HBzd2yrZnXyZZRqd25iYYPzZZk> NITkN45KdiC4aYTyc{BqdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhcHWvYX6gWE1k\WyuIIDyc4xq\mW{YYTpc44tKEmFNUC9NE42KG6P Ml\GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwPzV|N{OzNUc,PzV|N{OzNVww[T5?
rat RBL2H3 cells M3nrUmZ2dmO2aX;uJIF{e2G7 MV:xOUBucW6| NFjpSY9CdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKHKjdDDSRmwzUDNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBFVlBvQmPBMYlv\HWlZXSgWG5HNWGucHjhJJBzd2S3Y4Tpc44heHKnaX7jeYJifGWmIH\vdkAyPSCvaX7zJJBzcW:{IFTOVE1DW0FiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMh[nliRVzJV2EtKEmFNUC9NE4zPSCwTR?= Moq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2MUCwPFQoRjJ{NEGwNFg1RC:jPh?=
rat RBL2H3 cells MX\GeY5kfGmxbjDhd5NigQ>? MkHuNVYhcA>? MmPrTY5pcWKrdHnvckBw\iCWTl[tZYxxcGFicILv[JVkfGmxbjDpckBz[XRiUlLMNmg{KGOnbHzzJIFnfGW{IEG2JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjJ3IH7N MkfiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUGwO|YoRjJ|N{mxNFc3RC:jPh?=
PBMCs MmfISpVv[3Srb36gZZN{[Xl? NXTnZoRlUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEmITj3nZY1u[SCycn;keYN1cW:wIDjBcpRqNUOGMzDtc45w[2yxbnHsJIFvfGmkb3T5JJN1cW23bHH0[YQh[W6mIHP1cJR2emWmIFPEOEBxd3OrdHn2[UBk\WyuczDweZJq\mmnZDDmdo9uKGi3bXHuJJBmemmyaHXyZYwh[myxb3SgcY9vd263Y3zlZZIh[2WubDmsJGlEPTBiPTCwMlAxODB4IN88UU4> M2fsfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{[5N|k6Lz5zNUO2PVM6QTxxYU6=
PBMCs NUHSVGtkTnWwY4Tpc44h[XO|YYm= MVrJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTWwuPSCycn;keYN1cW:wIDjBcpRqNUOGMzDtc45w[2yxbnHsJIFvfGmkb3T5JJN1cW23bHH0[YQh[W6mIHP1cJR2emWmIFPEOEBxd3OrdHn2[UBk\WyuczDweZJq\mmnZDDmdo9uKGi3bXHuJJBmemmyaHXyZYwh[myxb3SgcY9vd263Y3zlZZIh[2WubDmsJGlEPTBiPTCwMlAxODB4IN88UU4> M2LWNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{[5N|k6Lz5zNUO2PVM6QTxxYU6=
T-cells M1HtcmZ2dmO2aX;uJIF{e2G7 M1\jXHRp\SClb33wc5Vv\CC5YYOgeIV{fGWmIH\vdkBqfHNiaX7obYJqfG:{eTDhZ5Rqfmm2eTDh[4FqdnO2IGStZ4VtdCCycn;sbYZmemG2aX;uJJV{cW6pIH31dolv\SC|cHzlcolkKFRvY3XscJMtKEmFNUCgQUAxNjByMEKg{txONg>? NXrWOIg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUC0OVA6QDdpPkGwOFUxQTh5PD;hQi=>
RBL-2H3 M{izTWZ2dmO2aX;uJIF{e2G7 NYfofVB{UW6qaXLpeIlwdiCxZjDEUnA4NUKVQTDhcpRq\2WwLXnu[JVk\WRiVF7GZYxxcGFicnXs[YF{\SCrbjDyZZQhWkKOLULIN{Bk\WyuczygTWM2OCB;IECuNFAxOjVizszNMi=> NHfu[ZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkmwNVY6Pid-MU[5NFE3QTZ:L3G+
Jurkat T MXjJcY12dm:|dYDwdoV{e2m4ZTDhd5NigQ>? NETqW|kyPSC2bzCzNEBucW6| M3niSmludXWwb4P1dJBz\XO|aY\lJIFkfGm4aYT5JIlvKFCPQT;pc45wdXmlaX6gd5RqdXWuYYTl[EBpfW2jbjDKeZJs[XRiVDDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCLTEKgdJJw\HWldHnvckBxemW2cnXheIVlKG[xcjCxOUB1dyB|MDDtbY5{KG[xbHzve4VlKGK7IGDNRU9qd26xbYnjbY4h[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgNVghfG9iMkCgbJJ{KGK7IFXMTXNCNCCLQ{WwJF0hOC5|NjFOwG0v MnXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MUKyNFQoRjJ6NEGyNlA1RC:jPh?=
HEK293 M2\HZmZ2dmO2aX;uJIF{e2G7 NFPtTo9VWF:WUlHOV3BQWlSHUkqgbY5pcWKrdHnvckBw\iCSaHHscI9q\GmwIIXweIFs\SBqUHjhcIxwcWSrbkqgNUB2VSliaX6gU2FVWC2FLXX4dJJme3OrbnegTGVMOjl|IHPlcIx{NCCLQ{WwJF0hOy55IN88UU4> M2Sw[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF2NUOwPVA4Lz5zNEWzNFkxPzxxYU6=
Jurkat T MUnBcpRqcW6obHHtcYF1d3K7IHHzd4F6 NYDtXFJ1OjBibXnudy=> M1HKWGFvfGlvaX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKFCPQT;pc45wdXmlaX6gd5RqdXWuYYTl[EBpfW2jbjDKeZJs[XRiVDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hUUxvMjDz[YNz\XSrb36gdJJmcW6ldXLheIVlKG[xcjCyNEBucW6|IH\vcIxwf2WmIHL5JHBOSS:rb37vcZlkcW5ic4TpcZVt[XSrb36gcYVie3W{ZXSgZYZ1\XJiMUKgbJJ{KGK7IFXMTXNCNCCLQ{WwJF0hPS56IN88UU4> NHnvR5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEWwPVU2Oid-Mki1NFk2PTJ:L3G+
Assay
Methods Test Index PMID
Western blot p-S6K(S371) / S6K / p-Erα(S167) / Erα ; p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3 ; GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin 29344249 23470533 26455952
Immunofluorescence Tom20 / JC-1 / ROS / NF-κB ; FKBP51 ; FKBP52 / p23 / hsp90 30294901 20796173
Growth inhibition assay Cell viability 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 (from reference)

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

Chemical Information

Molecular Weight 804.02
Formula

C44H69NO12

CAS No. 104987-11-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05120570 Not yet recruiting Drug: VIC- 1911 Acute Leukemia|Myelodysplastic Syndromes|Myeloproliferative Neoplasm|Lymphoma Masonic Cancer Center University of Minnesota February 2022 Phase 1|Phase 2
NCT05148715 Not yet recruiting Drug: Tacrolimus|Drug: Placebo Organ Transplant Failure or Rejection|Brain Death|Ischemic Reperfusion Injury Université de Sherbrooke|McMaster University January 2022 Phase 2
NCT05005221 Recruiting Behavioral: Automated text messages Kidney Transplant University of Michigan January 24 2022 Not Applicable
NCT04505878 Not yet recruiting Drug: Vitamin C Primary Graft Dysfunction|Lung Transplant; Complications University of Wisconsin Madison January 2022 Phase 2
NCT05152628 Not yet recruiting Drug: Tacrolimus granules Liver Transplantation|Kidney Transplantation Astellas Pharma China Inc.|Astellas Pharma Inc December 31 2021 Phase 4
NCT05153915 Not yet recruiting Drug: Tacrolimus granules Liver Transplantation|Kidney Transplantation Astellas Pharma China Inc.|Astellas Pharma Inc December 31 2021 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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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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