Tacrolimus (FK506)

Synonyms: FR900506, Fujimycin

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.

Tacrolimus (FK506) Chemical Structure

Tacrolimus (FK506) Chemical Structure

CAS: 104987-11-3

Selleck's Tacrolimus (FK506) has been cited by 89 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human U251 cells Function assay Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay, IC50=13.8 nM 17643112
human WiDr cells Growth inhibition assay Inhibition of SAP130 mediated cell growth in human WiDr cells, IC50=10.9 nM 17643112
human T-cell Proliferation assay In vitro inhibitory activity against human T-cell proliferation, IC50=0.5 nM 7537331
rat RBL2H3 cells Function assay 15 mins Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA, IC50=0.25 nM 22410084
rat RBL2H3 cells Function assay 16 h Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA, IC50=0.25 nM 23791076
PBMCs Function assay Inhibitory activity against IFN-gamma production (Anti-CD3 monoclonal antibody stimulated and cultured CD4 positive cells purified from human peripheral blood mononuclear cell), IC50 = 0.00006 μM. 15369399
PBMCs Function assay Inhibitory activity against IL-5 production (Anti-CD3 monoclonal antibody stimulated and cultured CD4 positive cells purified from human peripheral blood mononuclear cell), IC50 = 0.00006 μM. 15369399
T-cells Function assay The compound was tested for its inhibitory activity against T-cell proliferation using murine splenic T-cells, IC50 = 0.0002 μM. 10450987
RBL-2H3 Function assay Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells, IC50 = 0.00025 μM. 16901696
Jurkat T Immunosuppressive assay 15 to 30 mins Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA, IC50 = 0.36 μM. 28412204
HEK293 Function assay TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells, IC50 = 3.7 μM. 14530907
Jurkat T Antiinflammatory assay 20 mins Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA, IC50 = 5.8 μM. 28509552
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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
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 Research 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.

Experimental Result Images Methods Biomarkers Images PMID
Western blot GluA1 / pGluA1(S845) / GluA2 / GluA3 / Calcineurin p-JNK / JNK / p-ERK / ERK / Cytochrome c / cleaved caspase-3 p-S6K(S371) / S6K / p-Erα(S167) / Erα 26455952
Immunofluorescence FKBP52 / p23 / hsp90 FKBP51 Tom20 / JC-1 / ROS / NF-κB 20796173
Growth inhibition assay Cell viability 23470533
In Vivo
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]

Animal Research Animal Models Male C57BL/6J mice
Dosages 30 mg/kg
Administration Oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05432765 Not yet recruiting
Kidney Transplant Rejection
University of Florida
December 2024 Early Phase 1
NCT06147648 Not yet recruiting
Liver Transplantation
Beijing Tsinghua Chang Gung Hospital
December 1 2023 Phase 4
NCT05844527 Recruiting
Wound of Skin|Abdominal Wound
MedRegen LLC
November 20 2023 Phase 2
NCT06001320 Recruiting
Kidney Transplant; Complications|CMV
Virginia Commonwealth University|Merck Sharp & Dohme LLC
September 25 2023 Early Phase 1
NCT05955924 Recruiting
Non-melanoma Skin Cancer|Carcinoma Squamous Cell|Carcinoma Basal Cell|Keratinocyte Carcinoma
Women''s College Hospital|Canadian Institutes of Health Research (CIHR)|University Health Network Toronto|NOW Foods
August 28 2023 Phase 3
NCT05655273 Not yet recruiting
Liver Transplant Rejection|Immune System Suppression
University Health Network Toronto|Paladin Labs Inc.
June 1 2023 Phase 4

Chemical Information & Solubility

Molecular Weight 804.02 Formula

C44H69NO12

CAS No. 104987-11-3 SDF Download Tacrolimus (FK506) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (124.37 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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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. )

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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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