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Ascomycin, isolated from Streptomyces, suppresses immune response in vitro with IC50 of 0.55 nM for mouse mixed lymphocyte. Ascomycin inhibits calcineurin phosphatase with IC50 of 49 nM through formation of an FKBP12-FK520-calcineurin ternary complex. FK520 also accelerate the rate of nerve regeneration, and promotes neurite outgrowth. Ascomycin shows antimalarial effects via inhibition of the chaperone activity of this bifunctional protein.