1. Autophagy
  2. Autophagy

Tacrolimus (Synonyms: Fujimycin; FR900506; FK506)

Cat. No.: HY-13756 Purity: 98.46%
Handling Instructions

Tacrolimus binds to FK506 binding protein (FKBP). This complex inhibits calcineurin phosphatase (PP2B). Tacrolimus is a mTOR-independent autophagy inducer.

For research use only. We do not sell to patients.
Tacrolimus Chemical Structure

Tacrolimus Chemical Structure

CAS No. : 104987-11-3

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Other Forms of Tacrolimus:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


Tacrolimus binds to FK506 binding protein (FKBP). This complex inhibits calcineurin phosphatase (PP2B). Tacrolimus is a mTOR-independent autophagy inducer.

IC50 & Target

PP2B (calcineurin phosphatase)[1]
Autophagy inducer[2]

In Vitro

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]. Tacrolimus (FK506) is a powerful immunosuppressive drug widely used to prevent organ rejection after transplantation. Tacrolimus inhibit other calcineurin-dependent transcription factors including the ubiquitously expressed cAMP response element-binding protein (CREB). Tacrolimus inhibit CREB transcriptional activity at the coactivator level. The depolarization-induced transcriptional activity of the CBP C-terminus is enhanced by overexpression of calcineurin and is inhibited by Tacrolimus in a concentration-dependent manner with IC50 of 1 nM consistent with IC50 for inhibition of calcineurin[3].

In Vivo

In the pleurisy induced by carrageenan, Tacrolimus (1 mg/kg, i.p.) and Dexamethasone (0.5 mg/kg, i.p.) administered 0.5 h before causes a significant decrease in leukocytes, neutrophils and exudation (P<0.01). Under the same conditions, Tacrolimus and Dexamethasone do not modify the blood's white or red cells (P>0.05). Tacrolimus shows a long lasting antiinflammatory effect, inhibiting leukocytes and neutrophils for up to 24 h (P<0.01), whereas the inhibition of exudation is less marked (up to 2 h) (P<0.01). These drugs caused a marked reduction in MPO activity, as well as IL-1β and TNFα levels (P<0.01), but only Tacrolimus inhibits ADA activity (P<0.01). Tacrolimus significantly inhibits cell migration induces by either bradykinin, histamine or substance P (P<0.05)[4].

Clinical Trial
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.2438 mL 6.2188 mL 12.4375 mL
5 mM 0.2488 mL 1.2438 mL 2.4875 mL
10 mM 0.1244 mL 0.6219 mL 1.2438 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay

Tacrolimus (FK506) is dissolved in DMSO and stored, and then diluted with appropriate medium before use[3].

The pancreatic islet β-cell line HIT is grown in RPMI 1640 supplemented with 10% fetal calf serum, 5% horse serum, 100 U/mL Penicillin, and 100 μg/mL Streptomycin. HIT cells are transiently transfected by the DEAE-dextran method with 2 μg of indicator plasmid per 6-cm dish and 2 μg of expression vector per 6-cm dish, unless stated otherwise. Rous sarcoma virus-chloramphenicol acetyltransferase (0.5 μg per 6-cm dish) or cytomegalovirus green fluorescent protein expression vectors (1 μg per 6-cm dish) are added as second reporters to control for transfection efficiency. Cotransfections are carried out with a constant DNA concentration, which is maintained by adding the empty vector. Cells are stimulated with high KCl (final concentration 45 mM) or cAMP (forskolin 10 μM) 6 h before harvest, cyclosporin A or Tacrolimus are added 1 h before stimulation. Cell extracts are prepared 48 h after transfection. The chloramphenicol acetyltransferase assay and the luciferase assay are performed. Fluorescence of the green fluorescent protein is measured in a Packard FluoroCount with excitation wavelength at 485 nm and emission wavelength at 530 nm[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Tacrolimus (FK506) is dissolved in sterile saline (NaCl 0.9%) (Mice)[4].

Swiss mice, weighing 18-22 g, are randomly allocated in twelve groups: (1) Control-treated with sterile saline (NaCl, 0.9%, intrapleural route), (2) Cg (1%, ipl.), (3) Cg (1%, ipl.) plus Tacrolimus (0.5-1.5 mg/kg, i.p.), (4) Cg (1%, ipl.) plus dexametahasone (0.5 mg/kg, i.p.), (5) BK (10 nmol, ipl.), (6) BK (10 nmol, ipl.) plus Tacrolimus (1.0 mg/kg, i.p.), (7) Bradykinin (10 nmol, ipl.) plus Dexamethasone (0.5 mg/kg, i.p.), (8) Histamine (1 μg, ipl.), Histamine (1 μg, ipl.) plus Tacrolimus (1.0 mg/kg, i.p.), (9) Histamine (1 μg, ipl.) plus Dexamethasone (0.5 mg/kg, i.p.), (10) SP (20 nmol, ipl., (11), SP (20 nmol, ipl.) plus Tacrolimus (1.0 mg/kg, i.p.), and (12) SP (20 nmol, ipl.) plus Dexamethasone (0.5 mg/kg, i.p.). Tacrolimus and Dexamethasone are administered 0.5 h prior to pleurisy induction. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight







O=C([[email protected]@](CCCC1)([H])N1C(C([[email protected]@]2(O)[[email protected]](C)C[[email protected]](OC)[[email protected]@](O2)([H])[[email protected]@H](OC)C[[email protected]@H](C)C/C(C)=C/[[email protected]]3CC=C)=O)=O)O[[email protected]](/C(C)=C/[[email protected]]4C[[email protected]@H](OC)[[email protected]](O)CC4)[[email protected]](C)[[email protected]@H](O)CC3=O


4°C, protect from light

*The compound is unstable in solutions, freshly prepared is recommended.


Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 28 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.46%

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