Tacrolimus
Based on 106 publication(s) in Google Scholar
Tacrolimus (FK506), a molecular glue, a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 104987-11-3
- Formula: C44H69NO12
- Molecular Weight:804.02
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Publications Citing Use of MedChemExpress (MCE) Tacrolimus
More- Signal Transduct Target Ther. 2023 Nov 1;8(1):417. [Abstract]
- Mater Today. 2026 Apr 7;96:103326.
- Adv Funct Mater. 2023 Sep 15.
- J Extracell Vesicles. 2019 Dec 27;9(1):1709262. [Abstract]
- Exp Hematol Oncol. 2016 Jul 29:5:22. [Abstract]
- Theranostics. 2022 Jan 16;12(4):1621-1638. [Abstract]
- Theranostics. 2021 Mar 5;11(10):5045-5060. [Abstract]
- Theranostics. 2020 May 16;10(14):6483-6499. [Abstract]
- Theranostics. 2018 Jan 1;8(4):878-893. [Abstract]
- Biomaterials. 2021 May:272:120757. [Abstract]
- J Nanobiotechnology. 2025 Feb 4;23(1):81. [Abstract]
- J Control Release. 2020 Dec 10;328:237-250. [Abstract]
- Pharmacol Res. 2021 Feb:164:105382. [Abstract]
- Cell Mol Biol Lett. 2024 May 14;29(1):72. [Abstract]
- Mater Today Bio. 2024 Apr 22:26:101061. [Abstract]
- Cancer Lett. 2024 Jul 1:593:216841. [Abstract]
- Int J Biol Sci. 2024 Oct 7;20(14):5415-5435. [Abstract]
- J Colloid Interface Sci. 2023 Jan 15;630(Pt A):676-687. [Abstract]
- Burns Trauma. 2025 Feb 17:13:tkaf007. [Abstract]
- Acta Biomater. 2025 Apr:196:399-409. [Abstract]
- Proc Natl Acad Sci U S A. 2021 Jan 12;118(2):e2009539118. [Abstract]
- Nano Lett. 2019 Jan 9;19(1):124-134. [Abstract]
- Nano Res. 11, 6086-6101(2018).
- Cell Commun Signal. 2021 Oct 11;19(1):103. [Abstract]
- Int J Biol Macromol. 2024 Aug 3:134478. [Abstract]
- Acta Pharmacol Sin. 2024 May 17. [Abstract]
- Am J Transplant. 2023 Mar;23(3):336-352. [Abstract]
- Drug Deliv. 2021 Dec;28(1):1759-1768. [Abstract]
- Mater Design. 2023 Nov, 235, 112415.
- Hepatobiliary Surg Nutr. 2023 Dec 1;12(6):835-853. [Abstract]
- Br J Pharmacol. 2022 Jun;179(12):3078-3095. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Aging Dis. 2024 Feb 1;15(1):282-294. [Abstract]
- Cell Rep. 2021 Jul 20;36(3):109404. [Abstract]
- NPJ Regen Med. 2022 Sep 2;7(1):43. [Abstract]
- Elife. 2023 MAy 19.
- Fundam Res. 2024 Mar 19.
- J Agric Food Chem. 2025 Jun 18;73(24):14985-15002. [Abstract]
- Cell Biol Toxicol. 2022 Jun;38(3):487-504. [Abstract]
- Biomater Sci. 2023 May 30;11(11):4032-4042. [Abstract]
- Biomater Sci. 2020 Oct 7;8(19):5282-5292. [Abstract]
- Acta Physiol. 2026 Apr;242(4):e70189. [Abstract]
- Cell Prolif. 2023 Oct;56(10):e13460. [Abstract]
- ACS Biomater Sci Eng. 2022 Nov 14;8(11):4850-4862. [Abstract]
- J Ethnopharmacol. 2026 May 10:362:121364. [Abstract]
- Food Funct. 2023 Jul 31;14(15):7176-7194. [Abstract]
- Int J Pharm. 2025 Jan 20:125247. [Abstract]
- Int J Pharm. 2019 Dec 13;575:118951. [Abstract]
- Int J Mol Sci. 2024 Feb 21;25(5):2503. [Abstract]
- Int J Mol Sci. 2022 Aug 19;23(16):9376. [Abstract]
- Biomolecules. 2024 Jun 8;14(6):671. [Abstract]
- Eur J Pharmacol. 2026 Jun 25:1030:179091. [Abstract]
- Int Immunopharmacol. 2026 May 15:177:116529. [Abstract]
- Int Immunopharmacol. 2025 Sep 8:165:115459. [Abstract]
- Invest Ophthalmol Vis Sci. 2023 Jan 3;64(1):19. [Abstract]
- Hepatobiliary Pancreat Dis Int. 2024 Aug;23(4):344-352. [Abstract]
- Skelet Muscle. 2020 Apr 22;10(1):10. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2025 Apr 21;1871(6):167857. [Abstract]
- FASEB J. 2025 Apr 15;39(7):e70496. [Abstract]
- FASEB J. 2023 Feb;37(2):e22749. [Abstract]
- Mediators Inflamm. 2019 Dec 17;2019:4176974. [Abstract]
- Toxics. 2024 Aug 19;12(8):607. [Abstract]
- Antiviral Res. 2023 Jul:215:105618. [Abstract]
- J Neurochem. 2022 Dec;163(5):419-437. [Abstract]
- Toxins. 2019 Jun 18;11(6):349. [Abstract]
- Cell Signal. 2025 Sep 8:136:112116. [Abstract]
- J Cell Sci. 2019 May 20;132(10):jcs227777. [Abstract]
- Mol Med Rep. 2022 May;25(5):160. [Abstract]
- J Immunol. 2025 Dec 10:vkaf303. [Abstract]
- Vaccines. 2024 Sep 29;12(10):1117. [Abstract]
- Wound Repair Regen. 2023 Jul-Aug;31(4):489-499. [Abstract]
- Animal Model Exp Med. 2023 Jun;6(3):255-265. [Abstract]
- Dis Model Mech. 2019 Jan 28;12(1). pii: dmm036830. [Abstract]
- Pathol Res Pract. 2025 Aug:272:156095. [Abstract]
- J Pharm Biomed Anal. 2023 Oct 25:235:115652. [Abstract]
- Insect Sci. 2024 Jun;31(3):759-772. [Abstract]
- Clin Transl Sci. 2025 Feb;18(2):e70152. [Abstract]
- BMC Immunol. 2023 Nov 8;24(1):43. [Abstract]
- BMC Pharmacol Toxicol. 2022 Nov 28;23(1):87. [Abstract]
- Ultrasound Med Biol. 2023 Jul;49(7):1647-1657. [Abstract]
- Brain Res. 2019 May 15:1711:68-76. [Abstract]
- Acta Trop. 2020 Dec;212:105708. [Abstract]
- J Viral Hepat. 2026 Jan;33(1):e70118. [Abstract]
- Biochim Biophys Acta Gen Subj. 2022 Jun;1866(6):130133. [Abstract]
- J Toxicol Sci. 2024;49(8):337-348. [Abstract]
- Transpl Immunol. 2021 Oct:68:101434. [Abstract]
- J Vet Med Sci. 2023 Mar 30;85(4):443-446. [Abstract]
- Northwestern University. 2026.
- SSRN. 2026 May 28.
- Res Sq. 2026 Mar 27.
- Res Sq. 2025 Dec 17.
- bioRxiv. 2025 Nov 20.
- Seoul National University. 2033.
- Preprints. 2025 Sep 24.
- Developments and Experiments in Health and Medicine. 2025.
- Indiana University. 2025.
- bioRxiv. 2025 Jul 31:2025.07.30.667742. [Abstract]
- bioRxiv. 2025 February 01.
- Res Sq. 2024 Aug 13:rs.3.rs-4656461. [Abstract]
- SSRN. 2023 Oct 31.
- Hong Kong Polytechnic University. 2023 Apr.
- Patent. US20220087984A1.
- Research Square Preprint. 2020 Dec.
- Patent. US20180263995A1.
- Am J Dig Dis (Madison). 2015;2(2):95-99.
- Int J Physiol Pathophysiol Pharmacol. 2015 Mar 20;7(1):54-60. [Abstract]
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Biological Activity
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Macrolide |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B-cell | IC50 |
1.6 ng/mL
Compound: FK-506
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Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
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[PMID: 14738397] |
| B-cell | IC50 |
1.6 x 10-3 μg/mL
Compound: FK-506
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Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
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[PMID: 14738397] |
| CD4+ve Th | IC50 |
0.034 nM
Compound: 1; FK506
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Immunosuppressive activity in C57BL/6J mouse CD4+ve T cells assessed as inhibition of CD3/CD28-stimulated CD4+ve T cell proliferation incubated for 72 hrs by CellTrace-violet staining based flow cytometry analysis
Immunosuppressive activity in C57BL/6J mouse CD4+ve T cells assessed as inhibition of CD3/CD28-stimulated CD4+ve T cell proliferation incubated for 72 hrs by CellTrace-violet staining based flow cytometry analysis
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[PMID: 33534559] |
| HEK293 | IC50 |
3.7 μM
Compound: FK506
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TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells
TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells
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[PMID: 14530907] |
| HepG2 | IC50 |
>100 μM
Compound: 1; FK-506
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 28412204] |
| Jurkat | IC50 |
0.19 nM
Compound: FK-506
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Inhibitory activity against IL-2 receptor in human T-cell jurkat cell line stimulated by phytohemagglutininin and phorbol myristate acetate
Inhibitory activity against IL-2 receptor in human T-cell jurkat cell line stimulated by phytohemagglutininin and phorbol myristate acetate
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[PMID: 15369399] |
| Jurkat | IC50 |
0.36 μM
Compound: 1; FK-506
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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
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
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[PMID: 28412204] |
| Jurkat | IC50 |
5.8 μM
Compound: FK506
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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
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
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[PMID: 28509552] |
| Jurkat | IC50 |
0.056 nM
Compound: 1, FK506
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Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
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10.1039/C2MD20266B |
| PBMC | IC50 |
0.29 nM
Compound: FK-506
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Inhibitory activity against murine mixed lymphocyte reaction
Inhibitory activity against murine mixed lymphocyte reaction
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[PMID: 15369399] |
| RBL-2H3 | IC50 |
0.25 nM
Compound: FK-506
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Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells
Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells
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[PMID: 16901696] |
| RBL-2H3 | IC50 |
0.25 nM
Compound: FK-506
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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
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
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[PMID: 22410084] |
| RBL-2H3 | IC50 |
0.25 nM
Compound: FK506
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Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA
Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA
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[PMID: 23791076] |
| T-cell | IC50 |
1.5 x 10-5 μg/mL
Compound: FK-506
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Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation
Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation
|
[PMID: 11575965] |
| T-cell | IC50 |
1.5 x 10-5 μg/mL
Compound: FK-506
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Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
|
[PMID: 14738397] |
| T-cell | IC50 |
0.5 nM
Compound: FK-506
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In vitro inhibitory activity against human T-cell proliferation.
In vitro inhibitory activity against human T-cell proliferation.
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[PMID: 7537331] |
| T-cell | IC50 |
0.9 nM
Compound: FK-506
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In vitro inhibitory activity against human T-cell production of lymphokine IL-2
In vitro inhibitory activity against human T-cell production of lymphokine IL-2
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[PMID: 7537331] |
| T-cell | IC50 |
0.29 nM
Compound: 1 (FK-506)
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In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
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10.1016/S0960-894X(01)80264-X |
| T-cell | IC50 |
0.29 nM
Compound: 1 (FK-506)
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In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells
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10.1016/S0960-894X(01)80265-1 |
| T-cell | IC50 |
0.18 nM
Compound: 1 (FK-506)
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Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control
|
10.1016/S0960-894X(01)81248-8 |
| U-251 | IC50 |
13.8 nM
Compound: 1
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Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay
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[PMID: 17643112] |
| Vero 76 | IC50 |
>100 μM
Compound: 1; FK-506
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Cytotoxicity against African green monkey Vero 76 cells
Cytotoxicity against African green monkey Vero 76 cells
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[PMID: 28412204] |
| WiDr | IC50 |
10.9 nM
Compound: 1
|
Inhibition of SAP130 mediated cell growth in human WiDr cells
Inhibition of SAP130 mediated cell growth in human WiDr cells
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[PMID: 17643112] |
Tacrolimus (FK506) inhibits calcium-dependent events, such as IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance expression of the TGFβ-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by Tacrolimus[1]. Treatment with a low concentration of Tacrolimus (FK506,10 μg/L) does not significantly affect the proliferation of MH3924A cells (P=0.135). Upon treatment with higher concentrations of Tacrolimus (100-1,000 μg/L), the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100 μg/L), has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100 μg/L Tacrolimus, the in vitro proliferation of MH3924A cells is increased (P<0.01)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 104987-11-3
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Appearance Solid
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Molecular Weight 804.02
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Formula C44H69NO12
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Color White to off-white
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SMILES
O=C([C@@](CCCC1)([H])N1C(C([C@@]2(O)[C@H](C)C[C@H](OC)[C@@](O2)([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/[C@H]3CC=C)=O)=O)O[C@H](/C(C)=C/[C@H]4C[C@@H](OC)[C@H](O)CC4)[C@H](C)[C@@H](O)CC3=O
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Synonyms
FK506; Fujimycin; FR900506
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (106)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Immunity-and-matrix-regulatory cells enhance cartilage regeneration for meniscus injuries: a phase I dose-escalation trial. [Abstract]2023 Nov 1;8(1):417. PMID: 37907503 -
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J Extracell Vesicles
2019 Dec 27;9(1):1709262. PMID: 33133428
Tacrolimus purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2019 Dec 27;9(1):1709262. [Abstract]
Exosomal PD-L1 suppressed T cell activation and promoted skin cell migration in vitro (a). Representative confocal image show the appearance of exosomes as small-red dots. (b-c). Representative confocal images of pre-stained exosomes (red) colocalized with cell membrane (green) of HEK 293T (b) and Jurkat T cells (c).
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Exp Hematol Oncol
Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]2016 Jul 29:5:22. PMID: 27478685 -
Theranostics
Piezo1-mediated mechanosensation in bone marrow macrophages promotes vascular niche regeneration after irradiation injury. [Abstract]2022 Jan 16;12(4):1621-1638. PMID: 35198061 -
Theranostics
FGF19/SOCE/NFATc2 signaling circuit facilitates the self-renewal of liver cancer stem cells. [Abstract]2021 Mar 5;11(10):5045-5060. PMID: 33754043 -
Theranostics
STIM1 is a metabolic checkpoint regulating the invasion and metastasis of hepatocellular carcinoma. [Abstract]2020 May 16;10(14):6483-6499. PMID: 32483465 -
Theranostics
Sustained Release of Immunosuppressant by Nanoparticle-anchoring Hydrogel Scaffold Improved the Survival of Transplanted Stem Cells and Tissue Regeneration. [Abstract]2018 Jan 1;8(4):878-893. PMID: 29463988
Tacrolimus purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jan 1;8(4):878-893. [Abstract]
Accumulation of immune cells in host mice. Immunofluorescent images of CD4+ cells (green) in transplanted site in the normal, E+R, E+R+T, and E+R+T-RNPs groups at day 7 and day 21.
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Biomaterials
Targeted regulation of lymphocytic ER stress response with an overall immunosuppression to alleviate allograft rejection. [Abstract]2021 May:272:120757. PMID: 33798960 -
J Nanobiotechnology
RGD-HSA-TAC nanoparticles targeted delivery of tacrolimus and attenuation of podocyte injury in diabetic kidney disease. [Abstract]2025 Feb 4;23(1):81. PMID: 39905421 -
J Control Release
Target-oriented delivery of self-assembled immunosuppressant cocktails prolongs allogeneic orthotopic liver transplant survival. [Abstract]2020 Dec 10;328:237-250. PMID: 32866593 -
Pharmacol Res
2021 Feb:164:105382. PMID: 33348024 -
Cell Mol Biol Lett
lncRNA Oip5-as1 inhibits excessive mitochondrial fission in myocardial ischemia/reperfusion injury by modulating DRP1 phosphorylation. [Abstract]2024 May 14;29(1):72. PMID: 38745296 -
Mater Today Bio
3D in vitro synovial hyperplasia model on polycaprolactone-micropatterned nanofibrous microwells for screening disease-modifying anti-rheumatic drugs. [Abstract]2024 Apr 22:26:101061. PMID: 38711937 -
Cancer Lett
FPR3 reprograms glycolytic metabolism and stemness in gastric cancer via calcium-NFATc1 pathway. [Abstract]2024 Jul 1:593:216841. PMID: 38614385 -
Int J Biol Sci
Heterophyllin B enhances transcription factor EB-mediated autophagy and alleviates pyroptosis and oxidative stress after spinal cord injury. [Abstract]2024 Oct 7;20(14):5415-5435. PMID: 39494322 -
J Colloid Interface Sci
2023 Jan 15;630(Pt A):676-687. PMID: 36274404 -
Burns Trauma
Flufenamic acid inhibits pyroptosis in ischemic flaps via the AMPK-TRPML1-Calcineurin signaling pathway. [Abstract]2025 Feb 17:13:tkaf007. PMID: 40655077 -
Acta Biomater
Oral delivery of ultra-small zwitterionic nanoparticles to overcome mucus and epithelial barriers for macrophage modulation and colitis therapy. [Abstract]2025 Apr:196:399-409. PMID: 39983856 -
Proc Natl Acad Sci U S A
2021 Jan 12;118(2):e2009539118. PMID: 33376206 -
Nano Lett
2019 Jan 9;19(1):124-134. PMID: 30521345 -
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Cell Commun Signal
Zinc-mediated activation of CREB pathway in proliferation of pulmonary artery smooth muscle cells in pulmonary hypertension. [Abstract]2021 Oct 11;19(1):103. PMID: 34635097 -
Int J Biol Macromol
Nanoparticle-mediated calmodulin dsRNA and cyantraniliprole co-delivery system: High-efficient control of two key pear pests while ensuring safety for natural enemy insects. [Abstract]2024 Aug 3:134478. PMID: 39102908 -
Acta Pharmacol Sin
Restoration of HMGCS2-mediated ketogenesis alleviates tacrolimus-induced hepatic lipid metabolism disorder. [Abstract]2024 May 17. PMID: 38760545 -
Am J Transplant
miR-449a ameliorates acute rejection after liver transplantation via targeting procollagen-lysine1,2-oxoglutarate5-dioxygenase 1 in macrophages. [Abstract]2023 Mar;23(3):336-352. PMID: 36695693 -
Drug Deliv
Immunosuppressive effect of PLGA-FK506-NPs in treatment of acute cardiac rejection via topical subcutaneous injection. [Abstract]2021 Dec;28(1):1759-1768. PMID: 34463172 -
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Hepatobiliary Surg Nutr
Influence of immunosuppressive drugs on natural killer cells in therapeutic drug exposure in liver transplantation. [Abstract]2023 Dec 1;12(6):835-853. PMID: 38115918 -
Br J Pharmacol
Regenerating islet-derived protein 3 gamma (Reg3g) ameliorates tacrolimus-induced pancreatic β-cell dysfunction in mice by restoring mitochondrial function. [Abstract]2022 Jun;179(12):3078-3095. PMID: 35060126 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Aging Dis
ROR2-Related Skeletal Dysplasia Reveals Disrupted Chondrocyte Polarity through Modulation of BMP/TGF-β Signaling. [Abstract]2024 Feb 1;15(1):282-294. PMID: 37307827 -
Cell Rep
TRESK channel contributes to depolarization-induced shunting inhibition and modulates epileptic seizures. [Abstract]2021 Jul 20;36(3):109404. PMID: 34289346 -
NPJ Regen Med
Transplantation of PSC-derived myogenic progenitors counteracts disease phenotypes in FSHD mice. [Abstract]2022 Sep 2;7(1):43. PMID: 36056021 -
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J Agric Food Chem
FK506 Targets MoFpr1 to Modulate Autophagy and Ubiquitination, Inhibiting the Pathogenicity of Magnaporthe oryzae. [Abstract]2025 Jun 18;73(24):14985-15002. PMID: 40490869 -
Cell Biol Toxicol
Inhibition of calpain reduces cell apoptosis by suppressing mitochondrial fission in acute viral myocarditis. [Abstract]2022 Jun;38(3):487-504. PMID: 34365571
Tacrolimus purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2022 Jun;38(3):487-504. [Abstract]
FK506 inhibits dephosphorylation of Drp-1 at Ser637 site induced by CVB3 infection. CVB3 infection-induced decrease in Bcl-2 expression and enhanced levels of Bax and Caspase-3 cleavage are reversed by FK506.
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Biomater Sci
Electrospun polymer fibers modified with FK506 for the long-term treatment of acute cardiac allograft rejection in a heart transplantation model. [Abstract]2023 May 30;11(11):4032-4042. PMID: 37129635 -
Biomater Sci
Bioinspired β-glucan microcapsules deliver FK506 to lymph nodes for treatment of cardiac allograft acute rejection. [Abstract]2020 Oct 7;8(19):5282-5292. PMID: 32749395 -
Acta Physiol
Tacrolimus Induced Hypertension and Vascular Remodeling Includes Mechanisms of Cellular Senescence-The Protective Effect of Valsartan. [Abstract]2026 Apr;242(4):e70189. PMID: 41814130 -
Cell Prolif
WNT16b promotes the proliferation and self-renewal of human limbal epithelial stem/progenitor cells via activating the calcium/calcineurin A/NFATC2 pathway. [Abstract]2023 Oct;56(10):e13460. PMID: 36974338
Tacrolimus purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460. [Abstract]
FK506 (5 μM; 14 days) significantly inhibits the protein expression of both calcineurin A and NFATC2 in hLESCs.
Tacrolimus purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460. [Abstract]
FK506 (5 μM; 14 days) inhibits WNT16b on hLESC cell proliferation.
Tacrolimus purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460. [Abstract]
FK506 (5 μM; 14 days) significantly inhibits the expression of WNT16b-promoting cell proliferation marker Ki67 and the putative hLESC marker ΔNp63α in hLESCs.
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ACS Biomater Sci Eng
Mechanoresponsive Drug Loading System with Tunable Host-Guest Interactions for Ocular Disease Treatment. [Abstract]2022 Nov 14;8(11):4850-4862. PMID: 36214483 -
J Ethnopharmacol
Elephantopus scaber suppresses ConA-induced T cell activation by inhibiting NF-κB and Ca2+/NFAT signaling. [Abstract]2026 May 10:362:121364. PMID: 41687940 -
Food Funct
Sulforaphane protects microvascular endothelial cells in lower limb ischemia/reperfusion injury mice. [Abstract]2023 Jul 31;14(15):7176-7194. PMID: 37462424 -
Int J Pharm
Tannic acid-modified FK506-loaded nanoparticles targeting lymph nodes for acute heart transplant rejection treatment. [Abstract]2025 Jan 20:125247. PMID: 39842736 -
Int J Pharm
2019 Dec 13;575:118951. PMID: 31843550 -
Int J Mol Sci
Enhanced Diaphragm Muscle Function upon Satellite Cell Transplantation in Dystrophic Mice. [Abstract]2024 Feb 21;25(5):2503. PMID: 38473751 -
Int J Mol Sci
Expression of the Calcium-Binding Protein CALB1 Is Induced and Controls Intracellular Ca2+ Levels in Senescent Cells. [Abstract]2022 Aug 19;23(16):9376. PMID: 36012633 -
Biomolecules
Human Menstrual Blood-Derived Stem Cells Protect against Tacrolimus-Induced Islet Dysfunction via Cystathionine β-Synthase Mediated IL-6/STAT3 Inactivation. [Abstract]2024 Jun 8;14(6):671. PMID: 38927074 -
Eur J Pharmacol
Bergapten promotes angiogenesis by enhancing endothelial autophagy and reducing pyroptosis in ischemic skin flap. [Abstract]2026 Jun 25:1030:179091. PMID: 42349817 -
Int Immunopharmacol
2026 May 15:177:116529. PMID: 41871492 -
Int Immunopharmacol
Repurposing zafirlukast confers renal protection in ischemia-reperfusion injury via suppressing macrophage METosis. [Abstract]2025 Sep 8:165:115459. PMID: 40925201 -
Invest Ophthalmol Vis Sci
2023 Jan 3;64(1):19. PMID: 36692471 -
Hepatobiliary Pancreat Dis Int
HSP110 aggravates ischemia-reperfusion injury after liver transplantation by promoting NF-κB pathway. [Abstract]2024 Aug;23(4):344-352. PMID: 37648554 -
Skelet Muscle
Efficient engraftment of pluripotent stem cell-derived myogenic progenitors in a novel immunodeficient mouse model of limb girdle muscular dystrophy 2I. [Abstract]2020 Apr 22;10(1):10. PMID: 32321586 -
Biochim Biophys Acta Mol Basis Dis
IL-10 alleviates aTCMR by inhibiting NFATc1 signaling pathway of T cells after kidney transplantation. [Abstract]2025 Apr 21;1871(6):167857. PMID: 40268206 -
FASEB J
3,4-Dimethoxychalcone alleviates limb ischemia/reperfusion injury by TFEB-mediated autophagy enhancement and antioxidative response. [Abstract]2025 Apr 15;39(7):e70496. PMID: 40162605 -
FASEB J
2023 Feb;37(2):e22749. PMID: 36688808 -
Mediators Inflamm
Concomitant Treatment with Etanercept and Tacrolimus Synergistically Attenuates Arthritis Progression via Inhibition of Matrix Metalloproteinase-3 Production and Osteoclastogenesis in Human TNF- α Transgenic Mice. [Abstract]2019 Dec 17;2019:4176974. PMID: 31949424 -
Toxics
Evaluation of THP-1 and Jurkat Cell Lines Coculture for the In Vitro Assessment of the Effects of Immunosuppressive Substances. [Abstract]2024 Aug 19;12(8):607. PMID: 39195709
Tacrolimus purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607. [Abstract]
Tacrolimus monohydrate (100 nM-10 µM) decreased IL-2 secretion from Jurkat cells and coculture with THP-1 cells.
Tacrolimus purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607. [Abstract]
Tacrolimus monohydrate (100 nM-10 µM) caused significant TNFα inhibition in Jurkat cells and coculture with THP-1 cells.
Tacrolimus purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607. [Abstract]
Tacrolimus monohydrate (100 nM-10 µM) significantly inhibited IL-8 secretion from THP-1, Jurkat cells and their coculture.
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Antiviral Res
Codelivery of Cas9 mRNA and guide RNAs edits hepatitis B virus episomal and integration DNA in mouse and tree shrew models. [Abstract]2023 Jul:215:105618. PMID: 37142191 -
J Neurochem
Continued P2X7 activation leads to mitochondrial fission and compromising microglial phagocytosis after subarachnoid haemorrhage. [Abstract]2022 Dec;163(5):419-437. PMID: 36269673 -
Toxins
2019 Jun 18;11(6):349. PMID: 31216655 -
Cell Signal
Inhibition of ferroptosis rescues BMP osteogenic differentiation impaired by iron overload in the osteoporotic microenvironment. [Abstract]2025 Sep 8:136:112116. PMID: 40930476 -
J Cell Sci
FKBP12 mediates necroptosis by initiating RIPK1-RIPK3-MLKL signal transduction in response to TNF receptor 1 ligation. [Abstract]2019 May 20;132(10):jcs227777. PMID: 31028177 -
Mol Med Rep
P2X7 receptor knockdown suppresses osteoclast differentiation by inhibiting autophagy and Ca2+/calcineurin signaling. [Abstract]2022 May;25(5):160. PMID: 35266012 -
J Immunol
2025 Dec 10:vkaf303. PMID: 41369981 -
Vaccines
Comparative Ability of Various Immunosuppressants as Adjuvants on the Activity of T1D Vaccine. [Abstract]2024 Sep 29;12(10):1117. PMID: 39460283 -
Wound Repair Regen
Drug suspending during wound healing effectively weakens immunosuppression-related complications by preserving CD8+ T cell function. [Abstract]2023 Jul-Aug;31(4):489-499. PMID: 37129099 -
Animal Model Exp Med
Anti-inflammatory effects of amarogentin on 2,4-dinitrochlorobenzene-induced atopic dermatitis-like mice and in HaCat cells. [Abstract]2023 Jun;6(3):255-265. PMID: 36131559 -
Dis Model Mech
Yeast-model-based study identified myosin- and calcium-dependent calmodulin signalling as a potential target for drug intervention in chorea-acanthocytosis. [Abstract]2019 Jan 28;12(1). pii: dmm036830. PMID: 30635263 -
Pathol Res Pract
Combined treatment of tacrolimus and pirfenidone effectively improves BLM-induced pulmonary fibrosis in mice by inhibiting the TGFβ1/Smad2/3 signaling. [Abstract]2025 Aug:272:156095. PMID: 40617191 -
J Pharm Biomed Anal
Determination of five mTOR inhibitors in human plasma for hepatocellular carcinoma treatment using QuEChERS-UHPLC-MS/MS. [Abstract]2023 Oct 25:235:115652. PMID: 37633163 -
Insect Sci
Cytoplasmic FKBPs are involved in molting and metamorphosis through regulating the nuclear localization of EcR. [Abstract]2024 Jun;31(3):759-772. PMID: 37822278 -
Clin Transl Sci
2025 Feb;18(2):e70152. PMID: 39921332 -
BMC Immunol
Tacrolimus reverses pemphigus vulgaris serum-induced depletion of desmoglein in HaCaT cells via inhibition of heat shock protein 27 phosphorylation. [Abstract]2023 Nov 8;24(1):43. PMID: 37940861 -
BMC Pharmacol Toxicol
The effect of tacrolimus-induced toxicity on metabolic profiling in target tissues of mice. [Abstract]2022 Nov 28;23(1):87. PMID: 36443830 -
Ultrasound Med Biol
Amplification of Plasma MicroRNAs for Non-invasive Early Detection of Acute Rejection after Heart Transplantation With Ultrasound-Targeted Microbubble Destruction. [Abstract]2023 Jul;49(7):1647-1657. PMID: 37120328 -
Brain Res
Dephosphorylation by calcineurin regulates translocation of dynamin-related protein 1 to mitochondria in hepatic ischemia reperfusion induced hippocampus injury in young mice. [Abstract]2019 May 15:1711:68-76. PMID: 30659828
Tacrolimus purchased from MedChemExpress. Usage Cited in: Brain Res. 2019 May 15:1711:68-76. [Abstract]
Levels of CytC in cytosol (Cyto-CytC), CytC in mitochondria (Mito- CytC) and cleaved caspase-3 in hippocampus are determined by western blot with the treatment of sham, HIR, MDV or FK506.
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Acta Trop
Tacrolimus, a rapamycin target protein inhibitor, exerts anti-cystic echinococcosis effects both in vitro and in vivo. [Abstract]2020 Dec;212:105708. PMID: 32956634 -
J Viral Hepat
The Differential Effects of Immunosuppressants on Hepatitis E Virus Replication and the Triggered Inflammatory Responses in Macrophages. [Abstract]2026 Jan;33(1):e70118. PMID: 41400072 -
Biochim Biophys Acta Gen Subj
miR-731 modulates the zebrafish heart morphogenesis via targeting Calcineurin/Nfatc3a pathway. [Abstract]2022 Jun;1866(6):130133. PMID: 35346765 -
J Toxicol Sci
Validation of a new protocol for a zebrafish MEFL (malformation or embryo-fetal lethality) test method that conforms to the ICH S5 (R3) guideline. [Abstract]2024;49(8):337-348. PMID: 39098043 -
Transpl Immunol
Diphenyleneiodonium ameliorates acute liver rejection during transplantation by inhibiting neutrophil extracellular traps formation in vivo. [Abstract]2021 Oct:68:101434. PMID: 34216758 -
J Vet Med Sci
Detection of anti-feline infectious peritonitis virus activity of a Chinese herb extract using geneLEAD VIII, a fully automated nucleic acid extraction/quantitative PCR testing system. [Abstract]2023 Mar 30;85(4):443-446. PMID: 36806247 -
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bioRxiv
Cannabidiol exerts anti-inflammatory effects but maintains T effector memory cell differentiation: A Single-Cell Study in Humans. [Abstract]2025 Jul 31:2025.07.30.667742. PMID: 40766582 -
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Res Sq
Pharmacokinetics and Pharmacogenomics of Ribociclib in Black Patients with Metastatic Breast Cancer: The LEANORA study. [Abstract]2024 Aug 13:rs.3.rs-4656461. PMID: 39184092 -
Tacrolimus purchased from MedChemExpress. Usage Cited in: SSRN. 2023 Oct 31.
Tacrolimus monohydrate (FK506) (100 ng/mL) significantly increased the expressions of protein K14, CDH1 in kCSTA cells in an inflammatory environment.
Tacrolimus purchased from MedChemExpress. Usage Cited in: SSRN. 2023 Oct 31.
Tacrolimus monohydrate (FK506) (100 ng/mL) increased CSTA proteins in kCSTA cells.
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Int J Physiol Pathophysiol Pharmacol
The mTOR inhibitor sirolimus suppresses renal, hepatic, and cardiac tissue cellular respiration. [Abstract]2015 Mar 20;7(1):54-60. PMID: 26069529
Solvent & Solubility
DMSO : 125 mg/mL (155.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 12.5 mg/mL (15.55 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.11 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Tumor cell proliferation is determined by the MTT assay. Briefly, after MH3924A cells have reached the logarithmic growth phase, a 0.2-mL cell suspension at 1×104 cells/mL is added into each well of a 96-well plate and cultured in DMEM for 24 h. When adherent growth is established, different concentrations of Tacrolimus (10, 100 and 1,000 μg/L) , AMD3100 (10, 50 and 100 μg/L) and Tacrolimus (0 and 100 μg/L)+AMD3100 (0, 10, 50 and 100 μg/L) are added into the plates. Untreated cells cultured in medium alone are used as controls. After culturing for 48 h, 10 μL MTT (5 g/L) are added, and each well is incubated for 6 h; next, 150 μL/well DMSO are added, followed by measurements of the absorbance at 570 mm on a spectrophotometer reader. Each well is measured three times, and each sample is assayed in triplicate[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[4]
Six-week-old male C57BL/6J mice are maintained in a temperature- and humidity-controlled room with a 12-h light-dark cycle. For the multiple dosing study, colitic mice (n=10) are orally administered Tacrolimus at 30 mg/kg for 7 d (Days 10 to 16) or 14 d (Days 10 to 23). Control (n=10) and normal groups (n=5) are administered placebo using the same regimen. Tacrolimus or placebo is administered at 10 mL/kg. Mice are euthanized by CO2 inhalation on the day following the final dosing. For the single dosing study, colitic mice are orally administered Tacrolimus at 30 mg/kg or placebo (n=8) once on Day 7, 10, 17, or 24. Normal mice (n=4) are administered placebo using the same regimen. Mice are euthanized by CO2 inhalation eight hours after dosing[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (288 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Handling Instructions (2659 KB)
References
[1]. Thomson AW, et al. Mode of action of Tacrolimus (FK506): molecular and cellular mechanisms. Ther Drug Monit. 1995 Dec;17(6):584-91. [Content Brief]
[2]. Vogel KR, et al. mTOR inhibitors rescue premature lethality and attenuate dysregulation of GABAergic/glutamatergic transcription in murine succinate semialdehyde dehydrogenase deficiency (SSADHD), a disorder of GABA metabolism. J Inherit Metab Dis. 2016 Nov;39(6):877-886. [Content Brief]
[3]. Zhu H, et al. Tacrolimus promotes hepatocellular carcinoma and enhances CXCR4/SDF 1α expression in vivo. Mol Med Rep. 2014 Aug;10(2):585-92. [Content Brief]
[4]. Okada Y, et al. Tacrolimus ameliorates dextran sulfate sodium-induced colitis in mice: implication of interleukin-1β suppression. Biol Pharm Bull. 2011;34(12):1823-7. [Content Brief]
[6]. Soini L, et al. Molecular glues to stabilise protein-protein interactions. Curr Opin Chem Biol. 2022 Aug;69:102169. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 1.2438 mL | 6.2188 mL | 12.4375 mL | 31.0938 mL |
| 5 mM | 0.2488 mL | 1.2438 mL | 2.4875 mL | 6.2188 mL | |
| 10 mM | 0.1244 mL | 0.6219 mL | 1.2438 mL | 3.1094 mL | |
| 15 mM | 0.0829 mL | 0.4146 mL | 0.8292 mL | 2.0729 mL | |
| DMSO | 20 mM | 0.0622 mL | 0.3109 mL | 0.6219 mL | 1.5547 mL |
| 25 mM | 0.0498 mL | 0.2488 mL | 0.4975 mL | 1.2438 mL | |
| 30 mM | 0.0415 mL | 0.2073 mL | 0.4146 mL | 1.0365 mL | |
| 40 mM | 0.0311 mL | 0.1555 mL | 0.3109 mL | 0.7773 mL | |
| 50 mM | 0.0249 mL | 0.1244 mL | 0.2488 mL | 0.6219 mL | |
| 60 mM | 0.0207 mL | 0.1036 mL | 0.2073 mL | 0.5182 mL | |
| 80 mM | 0.0155 mL | 0.0777 mL | 0.1555 mL | 0.3887 mL | |
| 100 mM | 0.0124 mL | 0.0622 mL | 0.1244 mL | 0.3109 mL |
Tacrolimus Related Classifications
HY-13756 Related Classifications
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