| 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). |
| In vitro | 方法：胶质瘤细胞 C6 用 Cyclosporin A (10 μM) 在缺氧条件下处理 4 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：4 h 缺氧诱导了内源性 HIF-1α 蛋白的大量积累。Cyclosporin A 阻止了缺氧诱导的 HIF-1α 的大部分稳定。[1]方法：人结肠癌细胞 CACO-2 用 Cyclosporin A (2 μM) 处理 24-72 h，使用 Flow Cytometry 检测细胞周期情况。结果：在用 Cyclosporin A 处理后的 G0/G1 阶段检测到细胞的积聚。[2] |
| In vivo | 方法：为检测体内对肌肉疾病的活性，将 Cyclosporin A (5 mg/kg in olive oil) 腹腔注射给肌病 Col6a1-/- 小鼠，每天两次，持续十天。结果：Cyclosporin A 影响 Col6a1-/- 小鼠的卫星细胞活性并触发再生纤维的形成。[3]方法：为检测对缺血再灌注损伤 (IRI) 的作用，将 Cyclosporin A (3 mg/kg，在缺血前 1 h 或 10 min；10 mg/kg，在缺血前 10 min) 腹腔注射给缺血再灌注的 C57BL/6J 小鼠。结果：Cyclosporin A 10 mg/kg-10 min 和 Cyclosporin A 3 mg/kg-1 h 组的死亡率和肾功能显著高于 Cyclosporin A 3 mg/kg-10 min 组。[4] |
| Cell experiments | 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) |
| Target activity | Calcineurin phosphatase:7 nM |
| Synonyms | 环孢素, Cyclosporine A, Ciclosporin, Cyclosporine, 环孢菌素 |
| molecular weight | 1202.61 |
| Molecular formula | C62H111N11O12 |
| CAS | 59865-13-3 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (49.89 mM) Ethanol: 60.1 mg/mL (50 mM) |
| References | 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 7. Zheng B X, Long W, Zheng W, et al.Mitochondria-Selective Dicationic Small-Molecule Ligand Targeting G-Quadruplex Structures for Human Colorectal Cancer Therapy.Journal of Medicinal Chemistry.2024 |