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- Tacrolimus (FK506)
Tacrolimus (FK506)
Tacrolimus (FK506) is a potent and selective inhibitor of T-lymphocyte and the macrolide immunosuppressant [1].
In vitro, Tacrolimus (FK506) has been reported to inhibit the interleukin 2(IL-2) production and the response of mixed lymphocyte culture. In addition, Tacrolimus (FK506) added to the cell cultures has been revealed to inhibit murine or human mixed lymphocyte reactivity and the generation of cytotoxic T cells. Furermor, Tacrolimus (FK506) has also been reported to dose-dependently suppress the production of various cytokines including IL-2, IL-3, IL-4, and γ-interferon, in response to different stimulis. Besides, Tacrolimus has shown its efficacy in the prevention of allograft rejection in animal transplant models. Tacrolimus has been found to be significantly efficient in experimental hepatic allografts, and has hepatotrophic properties [1].
References:
[1] Wallemacq PE1, Reding R. FK506 (tacrolimus), a novel immunosuppressant in organ transplantation: clinical, biomedical, and analytical aspects. Clin Chem. 1993 Nov; 39(11 Pt 1):2219-28.
- 1. PENGYU JIA, NAN WU, et al. "Different roles of BAG3 in cardiac physiological hypertrophy and pathological remodeling." Transl Res. 2021 Jul;233:47-61. PMID:33578031
- 2. Carsten Deppermann, Moritz Peiseler, et al. "Tacrolimus impairs Kupffer cell capacity to control bacteremia: why transplant recipients are susceptible to infection." Hepatology. 2020 Aug 6. PMID:32761929
- 3. Souvik Dey, Alaa Eisa, et al. "Roles of glycogen synthase kinase 3 alpha and calcineurin in regulating the ability of sperm to fertilize eggs." FASEB J. 2020;34(1):1247–1269. PMID:31914663
- 4. Peiffer BJ, Qi L, et al. "Activation of BMP Signaling by FKBP12 Ligands Synergizes with Inhibition of CXCR4 to Accelerate Wound Healing." Cell Chem Biol. 2019 May 16;26(5):652-661.e4. PMID:30827938
- 5. Wang Z, Wang Y, et al. "Transient receptor potential channel 1/4 reduces subarachnoid hemorrhage-induced early brain injury in rats via calcineurin-mediated NMDAR and NFAT dephosphorylation." Sci Rep. 2016 Sep 19;6:33577. PMID:27641617
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 804.02 |
| Cas No. | 104987-11-3 |
| Formula | C44H69NO12 |
| Solubility | ≥26.6 mg/mL in DMSO; insoluble in H2O; ≥84.5 mg/mL in EtOH |
| SDF | Download SDF |
| Canonical SMILES | CO[C@@H]1C[C@H](/C=C(C)/[C@@H](OC([C@]2([H])CCCCN2C(C([C@]3(O)O[C@H]([C@@H](OC)C[C@H](C/C(C)=C/4)C)[C@@H](OC)C[C@H]3C)=O)=O)=O)[C@H](C)[C@H](CC([C@@H]4CC=C)=O)O)CC[C@H]1O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment: | |
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Cell lines |
Liver slices, human lung fibroblasts |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
2 μM and 4 μM for 3 days |
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Applications |
FK506 reduced type I collagen synthesis in liver slices cultured in vitro [1]. Moreover, FK506 (2 μM) decreased the type I collagen protein synthesis without affecting expression of collagen mRNAs [2]. |
| Animal experiment: | |
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Animal models |
Rats model |
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Dosage form |
4 mg/kg; i.p. injections, daily dose for 4 weeks; or 1, 2 and 3 mg/kg, p.o. for 10 consecutive days |
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Applications |
FK506 (4 mg/kg) prevented early stages of ethanol induced hepatic fibrosis by targeting LARP6 dependent mechanism of collagen synthesis in rats [1]. Moreover, FK506 (2 and 3 mg/kg) treatment resulted in attenuation of arterial ischemic reperfusion (I/R) induced axonal degeneration and histopathological alterations in rats [2]. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1Manojlovic, Z., Blackmon, J. and Stefanovic, B. (2013) Tacrolimus (FK506) prevents early stages of ethanol induced hepatic fibrosis by targeting LARP6 dependent mechanism of collagen synthesis. PLoS One. 8, e65897 2Muthuraman, A. and Sood, S. (2010) Pharmacological evaluation of tacrolimus (FK-506) on ischemia reperfusion induced vasculatic neuropathic pain in rats. J Brachial Plex Peripher Nerve Inj. 5, 13 |
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| Description | FK-506, a 23-membered macrolide lactone, is an inhibitor of peptidyl-prolyl isomerase. | |||||
| Targets | peptidyl-prolyl isomerase | |||||
| IC50 | ||||||
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