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Immunosuppressant
Cyclosporin A (CsA) is an immunosuppressant that has revolutionized organ transplantation through its use in the prevention of graft rejection. CsA binds to cyclophilin and suppresses its proline rotamase activity. The CsA-cyclophilin complex inhibits calcineurin, a type 2B phosphatase. It is an important diagnostic tool for the characterization of permeability transition-related phenomena. It inhibits mitochondrial permeability transition pore opening however, pore inhibition becomes less efficient at increasing Ca2+ loads and inhibition is transient. Inhibits staurosporin-induced apoptosis in cultured neural cells and rotenone-induced apoptosis in PC-12 cells. Inhibits cytochrome c release from mitochondria. Inhibits nitric oxide (NO) synthesis.
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Product Details
| Alternative Name |
CsA |
|---|---|
| Appearance |
White to off-white powder. |
| CAS |
59865-13-3 |
| Couple Target |
NOS, Serine/threonine-protein phosphatase |
| Couple Type |
Inhibitor |
| Formula |
C62H111N11O12 |
| MW |
1202.6 |
| Purity |
≥98% (Assay) |
| Solubility |
Soluble in DMSO (25mg/ml), methanol, 100% ethanol (25mg/ml), acetone or petroleum ether; insoluble in water. |
| Source |
Isolated from Fusarium solani |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months. |
|---|---|
| Long Term Storage |
-20°C |
| Shipping |
Ambient Temperature |
| Regulatory Status |
RUO – Research Use Only |
|---|
- Zebrafish Larvae Position Tracker (Z-LaP Tracker): a high-throughput deep-learning behavioral approach for the identification of calcineurin pathway-modulating drugs using zebrafish larvae: S.V. Gore, et al.; Sci. Rep. 13, 3174 (2023), Abstract
- Inhibition of pyruvate dehydrogenase kinase 4 in CD4+ T cells ameliorates intestinal inflammation: H. Lee, et al.; Cell. Mol. Gastroenterol. Hepatol. 15, 439 (2023), Abstract
- Shigella induces epigenetic reprogramming of zebrafish neutrophils: Gomes, M. C., Brokatzky, D., et al.; Sci. Adv. 9, eadf9706 (2023), Abstract
- Shigella induces epigenetic reprogramming of zebrafish neutrophils: Gomes, M. C., Brokatzky, D., et al.; bioRxiv , (2022)
- Novel use of FDA-approved drugs identified by cluster analysis of behavioral profiles: S.T. Edmister, et al.; Sci. Rep. 12, 6120 (2022), Abstract
- Lysophosphatidic Acid Promotes the Expansion of Cancer Stem Cells via TRPC3 Channels in Triple-Negative Breast Cancer: N. Hirata, et al.; Int. J. Mol. Sci. 23, 1967 (2022), Abstract
- Oxidative bursts of single mitochondria mediate retrograde signaling toward the ER: D.M. Booth, et al.; Mol. Cell 81, 3866 (2021), Abstract — Full Text
- Nitrogen Trapping as a Therapeutic Strategy in Tumors with Mitochondrial Dysfunction: Madala, H. R., Helenius, I. T., et al.; Cancer Res. 80, 3492 (2020), Abstract
- Phosphorylation and inhibition of ceramide kinase by protein kinase C-β: Their changes by serine residue mutations: H. Takahashi, et al.; Cell Signal. 54, 59 (2018), Abstract
- Mitochondrial BK Channel Openers CGS7181 and CGS7184 Exhibit Cytotoxic Properties: B. Augustynek, et al.; Int. J. Mol. Sci. 19, E353 (2018), Abstract
- Subcellular Distribution of HDAC1 in Neurotoxic Conditions Is Dependent on Serine Phosphorylation: Zhu, Y., Vidaurre, O. G., et al.; J. Neurosci. 37, 7547 (2017), Abstract
- Role of P-glycoprotein inhibitors in ceramide-based therapeutics for treatment of cancer: Morad, S. A. F., Davis, T. S., et al.; Biochem. Pharmacol. 130, 21 (2017), Abstract
- Differential induction of ATF3 and HO-1 in myeloid cells and keratinocytes via Dimethylfumarate or Cyclosporine A: S. Müller, et al.; J. Dermatol. Sci. 87, 246 (2017), Application(s): Treatment of human keratinocytes and PBMCs, Abstract
- Endotoxin tolerance in mast cells, its consequences for IgE-mediated signalling, and the effects of BCL3 deficiency: Poplutz, M., Levikova, M., et al.; Sci. Rep. 7, 4534 (2017), Abstract
- Monocyte Trafficking, Engraftment, and Delivery of Nanoparticles and an Exogenous Gene into the Acutely Inflamed Brain Tissue – Evaluations on Monocyte-Based Delivery System for the Central Nervous System: H.I. Tong, et al.; PLoS One 11, e0154022 (2016), Application(s): Cell culture, Abstract — Full Text
- Interactions of human P-glycoprotein transport substrates and inhibitors at the drug binding domain: Functional and molecular docking analyses: O. Kadioglu, et al.; Biochem. Pharmacol. 104, 42 (2016), Application(s): Cell culture, Abstract
- Mitotic phosphatase activity is required for MCC maintenance during the spindle checkpoint: Foss, K. M., Robeson, A. C., et al.; Cell Cycle 15, 225 (2015), Abstract
- Effects of embryonic cyclosporine exposures on brain development and behavior: D.E. Clift, et al.; Behav. Brain Res. 282, 117 (2015), Application(s): Cell Culture, Abstract
- 3D-Printed Drug/Cell Carrier Enabling Effective Release of Cyclosporin A for Xenogeneic Cell-Based Therapy: Song, T. H., Jang, J., et al.; Cell Transplant. 24, 2513 (2015), Abstract
- A small molecule with anticancer and antimetastatic activities induces rapid mitochondrial associated necrosis in breast cancer: A. Bastian, et al.; J. Pharmacol. Exp. Ther. 353, 392 (2015), Application(s): Assay, Abstract — Full Text
- Mouse Rankl expression is regulated in T cells by c-Fos through a cluster of distal regulatory enhancers designated the T cell control region: Bishop, K. A., Coy, H. M., et al.; J. Biol. Chem. 286, 20880 (2011), Abstract
- Phosphorylation of huntingtin at Ser421 in YAC128 neurons is associated with protection of YAC128 neurons from NMDA-mediated excitotoxicity and is modulated by PP1 and PP2A: Metzler, M., Gan, L., et al.; J. Neurosci. 30, 14318 (2010), Abstract
- Melatonin suppresses cyclosporine A-induced autophagy in rat pituitary GH3 cells: Y.M. Yoo & E.B. Jeung; J. Pineal Res. 48, 204 (2010), Abstract
- Prolonged infusion of inhibitors of calcineurin or L-type calcium channels does not block mossy fiber sprouting in a model of temporal lobe epilepsy: Ingram, E. A., Toyoda, I., et al.; Epilepsia 50, 56 (2009), Abstract
- The Bcl-2 family antagonist ABT-737 significantly inhibits multiple animal models of autoimmunity: Bardwell, P. D., Gu, J., et al.; J. Immunol. 182, 7482 (2009), Abstract
- Muscle-specific overexpression of the type 1 IGF receptor results in myoblast-independent muscle hypertrophy via PI3K, and not calcineurin, signaling: Quinn, L. S., Anderson, B. G., et al.; Am. J. Physiol. Endocrinol. Metab. 293, E1538 (2007), Abstract
- Chemokine fractalkine/CX3CL1 negatively modulates active glutamatergic synapses in rat hippocampal neurons: Ragozzino, D., Di Angelantonio, S., et al.; J. Neurosci. 26, 10488 (2006), Abstract
- Rationale for T cell inhibition by cyclosporin A in major autoimmune diseases: G.F. Ferraccioli, et al.; Ann. N. Y. Acad. Sci. 1051, 658 (2005), Abstract
- New aspects of cyclosporin a mode of action: from gene silencing to gene up-regulation: L. Mascarell & P. Truffa-Bachi; Mini. Rev. Med. Chem. 3, 205 (2003), Abstract
- Cyclosporin A binding to mitochondrial cyclophilin inhibits the permeability transition pore and protects hearts from ischaemia/reperfusion injury: A.P. Halestrap, et al.; Mol. Cell. Biochem. 174, 167 (1997), Abstract
- Immunological actions of cyclosporin A in rheumatoid arthritis: D. Yocum; Br. J. Rheumatol. 32 Suppl 1, 38 (1993), Abstract
- FK506 and ciclosporin: molecular probes for studying intracellular signal transduction: J. Liu; Trends. Pharmacol. Sci. 14, 182 (1993), Abstract
- Cyclosporin A, FK506 and rapamycin: more than just immunosuppression: J. Kunz & M.N. Hall; Trends. Biochem. Sci. 18, 334 (1993), Abstract
- Immunosuppression for organ grafting — observations on cyclosporin A: R.Y. Calne; Immunol. Rev. 46, 113 (1979), Abstract
- Cyclosporin A and C-New metabolites from Trichodermapolysporum: M. Dreyfuss, et al.; Europ. J. Appl. Microbiol. 3, 125 (1976)
- Cyclosporin A and C-New metabolites from Trichodermapolysporum: M. Dreyfuss, et al.; Europ. J. Appl. Microbiol. 3, 125 (1976)
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