Ascomycin
Ascomycin is an ethyl analog of FK506 that was initially produced by species of Streptomyces. Ascomycin binds FK506 binding protein 12 and the resulting complex inhibits calcineurin/protein phosphatase 2B (PP2B), altering peptidyl-prolyl isomerase activity of the enzyme. Ascomycin exhibits immunosuppressive, anti-inflammatory, and anticonvulsant activities. Clinically, ascomycin is used to treat organ transplant rejection and inflammatory skin diseases.
References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18842740
Cas No. |
104987-12-4 |
---|---|
Purity |
≥98% |
Formula |
C43H69NO12 |
Formula Wt. |
792.01 |
Melting Point |
162-163°C |
Solubility |
Soluble in DMSO |
Appearance |
White Powder |
Liu F, Wang YQ, Meng L, et al. FK506-binding protein 12 ligands: a patent review. Expert Opin Ther Pat. 2013 Nov;23(11):1435-49. PMID: 23957229.
Sierra-Paredes G, Sierra-Marcuño G. Ascomycin and FK506: pharmacology and therapeutic potential as anticonvulsants and neuroprotectants. CNS Neurosci Ther. 2008 Spring;14(1):36-46. PMID: 18482098.
Pahl A, Keller U. FK-506-binding proteins from streptomycetes producing immunosuppressive macrolactones of the FK-506 type. J Bacteriol. 1992 Sep;174(18):5888-94. PMID: 1381710.