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Cyclosporin A

Catalog No. T0945 CAS 59865-13-3

Synonyms: Cyclosporine A, Ciclosporin, Cyclosporine

Cyclosporin A is a naturally occurring cyclic polypeptide that is the active metabolite of a fungus. Cyclosporin A is an immunosuppressant that binds to procyclins and inhibits calcineurin (IC50=7 nM).

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Cyclosporin A, CAS 59865-13-3

Pack Size	Availability	Price/USD
50 mg	In stock	$ 36.00
100 mg	In stock	$ 50.00
200 mg	In stock	$ 66.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.85%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Cyclosporin A is a naturally occurring cyclic polypeptide that is the active metabolite of a fungus. Cyclosporin A is an immunosuppressant that binds to procyclins and inhibits calcineurin (IC50=7 nM).
Targets&IC50	Calcineurin phosphatase:7 nM
In vitro	METHODS: Glioma cell C6 was treated with Cyclosporin A (10 μM) under hypoxic conditions for 4 h. The expression levels of target proteins were measured by Western Blot. RESULTS: 4 h hypoxia induced a large accumulation of endogenous HIF-1α protein, and Cyclosporin A prevented most of the hypoxia-induced HIF-1α stabilization. [1] METHODS: Human colon cancer cells CACO-2 were treated with Cyclosporin A (2 μM) for 24-72 h. The cell cycle was detected by Flow Cytometry. RESULTS: Accumulation of cells was detected in the G0/G1 phase after treatment with Cyclosporin A. The RESULTS were summarized in the following table. [2]
In vivo	METHODS: To assay activity against muscle disease in vivo, Cyclosporin A (5 mg/kg in olive oil) was injected intraperitoneally into myopathic Col6a1-/- mice twice daily for ten days. RESULTS: Cyclosporin A affected satellite cell activity and triggered regenerative fiber formation in Col6a1-/- mice. [3] METHODS: To detect the effects on ischemia-reperfusion injury (IRI), Cyclosporin A (3 mg/kg, 1 h or 10 min before ischemia; 10 mg/kg, 10 min before ischemia) was intraperitoneally injected into ischemia-reperfused C57BL/6J mice. RESULTS: Mortality and renal function were significantly higher in the Cyclosporin A 10 mg/kg-10 min and Cyclosporin A 3 mg/kg-1 h groups than in the Cyclosporin A 3 mg/kg-10 min group. [4]
Kinase Assay	Phosphatase Assay: Purified bovine brain calcineurin and calmodulin are purchased. Reaction mixtures with purified enzyme contains 100 nM calcineurin, 100 nM calmodulin, and 5 μM 32P-labeled phosphopeptide, in 60 μl (total volume) of assay buffer containing 20 mM Tris (pH 8), 100 mM NaCI, 6 mM MgCl2, 0.5 mM dithiothreitol, 0.1 mg of bovine serum albumin per ml, and either 0.1 mM CaCl2 or 5 mM EGTA. Reaction mixtures with cell lysates contains 20 μl of undiluted lysate, 5 μM 32P-labeled phosphopeptide, and 40 μl of assay buffer. Where indicated, reaction mixtures contains 50 μM peptide 412 or 413 and/or 500 nM okadaic acid, a specific inhibitor of phosphatases 1 and 2A; 500 nM okadaic acid is sufficient for inhibition of Ca2+-independent phosphatases, whereas higher concentrations partially inhibit Ca2+-dependent activity as well. After 15 min at 30°C, reactions are terminated by the addition of 0.5 ml of 100 mM potassium phosphate buffer (pH 7.0) containing 5% trichloroacetic acid. Free inorganic phosphate is isolated by Dowex cation-exchange chromatography and quantitated by scintillation counting as described.
Cell Research	Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (106) are suspended in 1 ml of complete medium in microcentrifuge tubes; 1 μl of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 ml of PBS on ice and lysed in 50μl of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of aprotinin per ml. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g.(Only for Reference)

Synonyms	Cyclosporine A, Ciclosporin, Cyclosporine
Molecular Weight	1202.61
Formula	C62H111N11O12
CAS No.	59865-13-3

Storage

keep away from moisture

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

Solubility Information

DMSO: 120.3 mg/mL (100 mM)

Ethanol: 60.1 mg/mL (50 mM)

References and Literature

1. D'Angelo G, et al. Cyclosporin A prevents the hypoxic adaptation by activating hypoxia-inducible factor-1alpha Pro-564 hydroxylation. J Biol Chem. 2003 Apr 25;278(17):15406-11. 2. Werneck MB, et al. Cyclosporin A inhibits colon cancer cell growth independently of the calcineurin pathway. Cell Cycle. 2012 Nov 1;11(21):3997-4008. 3. Gattazzo F, et al. Cyclosporin A Promotes in vivo Myogenic Response in Collagen VI-Deficient Myopathic Mice. Front Aging Neurosci. 2014 Sep 15;6:244. 4. Lemoine S, et al. Dose and timing of injections for effective cyclosporine A pretreatment before renal ischemia reperfusion in mice. PLoS One. 2017 Aug 10;12(8):e0182358. 5. Nicolli A, et al. J Biol Chem, 1996, 271(4), 2185-2192. 6. Liu J, Giri B R, Chen Y, et al. Schistosoma japonicum IAP and Teg20 safeguard tegumental integrity by inhibiting cellular apoptosis[J]. PLoS neglected tropical diseases. 2018 Jul 25;12(7):e0006654. 7. Song J, Zou D, Zhao X, et al. Bufalin inhibits human diffuse large B-cell lymphoma tumorigenesis by inducing cell death through the Ca2+/NFATC1/cMYC pathway[J]. Carcinogenesis. 2020 8. Song J, Zou D, Zhao X, et al. Bufalin inhibits human diffuse large B cell lymphoma tumorigenesis by inducing cell death through the Ca 2+/NFATC1/cMYC pathway[J]. Carcinogenesis. 2020

Citations

1. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 2. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 3. Bao, Shixiang, et al. TGF-β1 Induces Immune Escape by Enhancing PD-1 and CTLA-4 Expression on T Lymphocytes in Hepatocellular Carcinoma. Frontiers in Oncology. 11 (2021): 2516. 4. Song J, Zou D, Zhao X, et al. Bufalin inhibits human diffuse large B-cell lymphoma tumorigenesis by inducing cell death through the Ca2+/NFATC1/cMYC pathway. Carcinogenesis. 2020 5. Liu J, Giri B R, Chen Y, et al. Schistosoma japonicum IAP and Teg20 safeguard tegumental integrity by inhibiting cellular apoptosis. PLoS Neglected Tropical Diseases. 2018 Jul 25;12(7):e0006654 6. Ren Y, Tong X, Zhao Y, et al. Dolabrane-Type Diterpenoids with Immunosuppressive Activity from Koilodepas hainanense. Journal of Natural Products. 2022

Related compound libraries

This product is contained In the following compound libraries：

Microbial Natural Product Library Drug Repurposing Compound Library Anti-Infection Compound Library Clinical Compound Library Glycometabolism Compound Library Pediatric Drug Library Approved Drug Library Toxic Compound Library Hematopoietic Toxicity Compound Library Metabolism Compound Library

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Keywords

Cyclosporin A 59865-13-3 Immunology/Inflammation Metabolism Microbiology/Virology Antibiotic Complement System Phosphatase CsA Ciclosporin A Cyclosporine A Ciclosporin Inhibitor Cyclosporine inhibit inhibitor

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