Description
Ascomycin (11011-38-4) is an analog of FK-506 (Cat.# 10-1103). Potent immunosuppressant1. Binds to FKBP122 and inhibits calcineurin and NFAT. Ascomycin displays anti-inflammatory effects in skin diseases3. Cell permeable and active in vivo.
Uses
A potent immunosuppressive agent and could be used as a potential therapeutic agent for autoimmune diseases.
General Description
An ethyl analog of FK506 with similar immunosuppressant properties. Acts by binding to immunophilins. Inhibits the synthesis of Th-1 and Th-2 type cytokines in target cells.
Biochem/physiol Actions
Product does not compete with ATP.
Enzyme inhibitor
This antifungal antibiotic (FW = 792.02 g/mol; CAS 104987-12-4;
Solubility: 50 mM in DMSO), also known as FK520, isolated from
Streptomyces hygroscopicus, is also a powerful immunosuppressant. Note
that ascomycin is a structural analogue of tacrolimus (or FK506) and, as
such, operates by a similar mechanism of action (See Tacrolimus).
Ascomycin inhibits allogenic T-lymphocyte proliferation and calcineurin
phosphatase activity.
References
1) Hatanaka et al. (1988), FR-900520 and FR-900523, novel immunosuppressants isolated from a Streptomyces. II. Fermentation, isolation and physio-chemical and biological characteristics; J. Antibiot. (Tokyo), 41 1592
2) Petros et al. (1991), NMR studies of an FK506 analogue [U-13C]ascomycin, bound to FKBP: conformation and regions of ascomycin involved in binding; J. Med. Chem., 34 2925
3) Mollison et al. (1999), A macrolactam inhibitor of T helper type 1 and T helper type 2 cytokine biosynthesis for topical treatment of inflammatory skin diseases; J. Invest. Dermatol., 112 729
