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Tacrolimus

Catalog No. T2144 CAS 104987-11-3

Synonyms: Fujimycin, FK506, FR900506

Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.

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Tacrolimus, CAS 104987-11-3

Pack Size	Availability	Price/USD
10 mg	In stock	$ 38.00
25 mg	In stock	$ 55.00
50 mg	In stock	$ 68.00
100 mg	In stock	$ 106.00
200 mg	In stock	$ 150.00
500 mg	In stock	$ 256.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 99.94%

Purity: 99.87%

Purity: 98.98%

Purity: 98.26%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.
Targets&IC50	FKBP12:0.2 nM (Kd)
In vitro	FKBP12 was first isolated from the cytosol of Jurkat T cells, as an abundant, high-affinity receptor for Tacrolimus (FK506; Kd: 0.2 nM) [1]. FK506 (100?1,000 μg/l) significantly promoted the proliferation of MH3924A cells. The invasiveness of MH3924A cells was significantly enhanced following treatment with FK506 [2]. FK506 specifically inhibits cellular calcineurin at drug concentrations that inhibit interleukin 2 productions in activated T cells [3].
In vivo	The liver of rats of the normal saline (NS) group was large, with an average weight at 15.56±11.17 g, and the liver of rats of the FK506 group was oversize, with an average weight at 28.19±3.89 g. The rate of lymph node metastasis, as well as the number of pulmonary nodules, were significantly increased in the FK506 compared to the NS group [2]. Behavioral pain assessment revealed an increase in the paw and tail withdrawal threshold in tacrolimus-treated groups against hyperalgesic and allodynic stimuli as compared to the sham control group [4].
Cell Research	Tumor cell proliferation was determined by the MTT. Briefly, after MH3924A cells had reached the logarithmic growth phase, a 0.2-ml cell suspension at 1×10^4 cells/ml was added into each well of a 96-well plate and cultured in DMEM with 10% FBS, 10 μg/l vascular endothelial growth factor and 0.1 g/l heparin for 24 h. When adherent growth was established, different concentrations of FK506 (10, 100 and 1,000 μg/l), AMD3100 (10, 50 and 100 μg/l) and FK506 (0 and 100 μg/l) + AMD3100 (0, 10, 50 and 100 μg/l) were added into the plates. Untreated cells cultured in medium alone were used as controls. After culturing for 48 h, 10 μl MTT (5 g/l) was added, and each well was incubated for 6 h; next, 150 μl/well dimethyl sulfoxide was added, followed by measurements of the absorbance at 570 mm on a spectrophotometer reader. Each well was measured three times, and each sample was assayed in triplicate [2].
Animal Research	Experiments were performed in 16 healthy August Copenhagen Irish rats (male, 16–20 weeks, weighing 240–300 g). The rat model of liver tumor was established as follows: First, MH3924A cells were collected and injected into the alar skin of rats. The tumors were removed from alar skin when grown to 2×1×1 mm3, and intrahepatic tumor implantation of rats was performed under aseptic conditions as described previously (25,26). Five days later, rats were randomly divided into two groups: one group was subcutaneously injected with normal saline for 14 days (NS group, n=8, 3 mg/kg/day), and the second group was subcutaneously injected with FK506 for 14 days (FK506 group, n=8, 0.3 mg/kg/day). Forty days following implantation, rats were sacrificed, and the weight of tumor, the volume of the fluid in the ascites, the incidence of lymphatic metastasis in the abdominal cavity and of abdominal wall metastasis were measured. In addition, the lungs were irrigated with 15% Indian ink, followed by counting of the number of metastatic nodules in the lung. The tumor and adjacent tissues, as well as healthy liver tissues, were harvested and preserved in 4% formalin for later use [2].

Synonyms	Fujimycin, FK506, FR900506
Molecular Weight	804.02
Formula	C44H69NO12
CAS No.	104987-11-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 80.4 mg/mL (100 mM)

DMSO: 80.4 mg/mL (100 mM)

References and Literature

1. Dumont FJ. FK506, an immunosuppressant targeting calcineurin function. Curr Med Chem. 2000 Jul;7(7):731-48. 2. 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. 3. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90. 4. Muthuraman A, Sood S. Pharmacological evaluation of tacrolimus (FK-506) on ischemia reperfusion induced vasculatic neuropathic pain in rats. J Brachial Plex Peripher Nerve Inj. 2010 Jun 7;5:13. 6. Yuwei He, et al. Drug targeting through platelet membrane-coated nanoparticles for the treatment of rheumatoid arthritis. Nano Res. 30 June 2018. 7. Wang W, Ren S, Lu Y, et al. Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production. The EMBO Journal. 2021: e106771.

Citations

1. Wang W, Ren S, Lu Y, et al. Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production. The EMBO Journal. 2021 Jun 1;40(11):e106771. doi: 10.15252/embj.2020106771. Epub 2021 Apr 28. 2. Chang Z, Zhang Q, Hu Q, et al. Tannins in Terminalia bellirica inhibits hepatocellular carcinoma growth via re-educating tumor-associated macrophages and restoring CD8+ T cell function. Biomedicine & Pharmacotherapy. 2022, 154: 113543. 3. Huang, Jing, et al. Osteopontin isoform c promotes the survival of cisplatin-treated NSCLC cells involving NFATc2-mediated suppression on calcium-induced ROS levels.. BMC cancer. 21.1 (2021): 1-14.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Kinase Inhibitor Library Microbial Natural Product Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library FDA-Approved Kinase Inhibitor Library Inhibitor Library Glycometabolism Compound Library

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Keywords

Tacrolimus 104987-11-3 Autophagy Metabolism Microbiology/Virology Others PI3K/Akt/mTOR signaling Phosphatase Antibacterial Antibiotic mTOR FKBP FK506-binding protein Inhibitor Fujimycin Bacterial FR-900506 FK 506 FK506 FK-506 inhibit FR 900506 FR900506 inhibitor

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