雷帕霉素被用作一种原始的抗真菌抗生素,由吸湿链霉菌生产。现在,由于其免疫抑制作用,它已被用于预防移植排斥反应。它还对几种可移植肿瘤具有活性,对白血病具有轻微的无活性活性。雷帕霉素的免疫抑制作用是通过抑制T细胞的活化和增殖来发挥的。雷帕霉素与 FK 结合蛋白 12 (FKBP12) 结合并形成雷帕霉素-FKBP12 复合物,该复合物调节一种在细胞周期进程中起重要作用的酶。
艾美捷APExBIO 原味抗真菌抗生素--雷帕霉素(西罗莫司)化学性质:
形态 固体
存储 在 -20°C 下干燥
分子量 914.18
CAS号 53123-88-9
公式 C51H79NO13
同义词 西罗莫司,(-)-雷帕霉素,AY-22989,WY-090217,抗生素AY22989
溶解度 ≥45.7 mg/mL 的 DMSO 溶液;不溶于H2O;≥58.9 mg/mL 的 EtOH 超声波溶液
运输条件 小分子与蓝冰,修饰核苷酸与干冰。
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APExBIO 原味抗真菌抗生素--雷帕霉素(西罗莫司)参考文献:
1. Sehgal, Suren N. "Rapamune?(RAPA, rapamycin, sirolimus): mechanism of action immunosuppressive effect results from blockade of signal transduction and inhibition of cell cycle progression." Clinical biochemistry 31.5 (1998): 335-340.
2. Sehgal, S. N., H. Baker, and Claude Vézina. "Rapamycin (AY-22,989), a new antifungal antibiotic. II. Fermentation, isolation and characterization." The Journal of antibiotics 28.10 (1975): 727-732.
APExBIO 原味抗真菌抗生素--雷帕霉素(西罗莫司)引用文献:
1. Weiran Li, Yuhui Yang, et al. "Autophagy mediates cementoblast mineralization through periostin/β-catenin signaling axis under compression." Research Square October 13th, 2022.
2. Yan Tang, David J. Kwiatkowski, et al. "Midkine expression by stem-like tumor cells drives persistence to mTOR inhibition and an immune-suppressive microenvironment." Nat Commun. 2022 Aug 26;13(1):5018. PMID: 36028490
3. Yang Liu, Libo He, et al. "Pharmacological inhibition of sphingolipid synthesis reduces ferroptosis by stimulating the HIF-1 pathway." iScience. 2022 Jun 6;25(7):104533. PMID: 35784791
4. Yogev Sela, Jinyang Li, et al. "Bcl-xL enforces a slow-cycling state necessary for survival in the nutrient-deprived microenvironment of pancreatic cancer." Cancer Res. 2022 May 16;82(10):1890-1908. PMID: 35315913
5. Zheng Zhang, Feng Zhang, et al. "CDC42 controlled apical-basal polarity regulates intestinal stem cell to transit amplifying cell fate transition via YAP-EGF-mTOR signaling." Cell Rep. 2022 Jan 11;38(2):110009. PMID: 35021092
6. Jordan E Hollembeak, Michael A Model. "Stability of Intracellular Protein Concentration under Extreme Osmotic Challenge." Cells. 2021 Dec 14;10(12):3532. PMID: 34944039
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