他克莫司相关化合物A | Ascomycin - MedChemExpress
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他克莫司相关化合物A
CAS No. : 104987-12-4
MCE 国际站:Ascomycin
产品活性:Ascomycin (Immunomycin; FR-900520; FK520) 是 Tacrolimus (FK506) 的乙基类似物,具有很强的免疫抑制特性。Ascomycin 也是一种大环聚酮类抗生素,具有抗疟疾、抗真菌和抗痉挛等多种生物活性。Ascomycin 可防止移植排斥,并具有用于各种皮肤病研究的潜力。
研究领域:Apoptosis | Immunology/Inflammation | Autophagy | Anti-infection
作用靶点:FKBP | Parasite | Fungal | Antibiotic
In Vitro: Ascomycin (FR-900520) suppresses immune response in vitro with an IC50 value of 0.55 nM for mouse mixed lymphocyte reaction.
Ascomycin is a powerful calcium-dependent serine/threonine protein phosphatase (calcineurin [CaN], protein phosphatase 2B) inhibitors. Its mechanism of action involves the formation of a molecular complex with the intracellular FK506-binding protein-12 (FKBP12), thereby acquiring the ability to interact with CaN and to interfere with the dephosphorylation of various substrates.
In Vivo: Ascomycin (FR-900520; i.m.; 0.32-32 mg/kg; 5 days a week; for 2 weeks) clearly prolongs skin allograft survival in rats.
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