Rapamycin (Sirolimus)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
雷帕霉素(Rapamycin)过去常被用作抗真菌类抗生素,是由Streptomyces hygroscopicus产生的。目前,由于Rapamycin的免疫抑制效应,其可用于预防移植排斥反应。Rapamycin还可以抑制几种移植性肿瘤,但对白血病只有轻微的甚至没有效果。Rapamycin通过抑制T细胞的激活和增殖而发挥免疫抑制作用。Rapamycin与FK结合蛋白12(FKBP12)结合形成rapamycin-FKBP12复合体,该复合体可以抑制mTOR。mTOR在细胞周期进程中发挥重要作用。
参考文献:
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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.
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Physical Appearance | A solid |
Storage | Desiccate at -20°C |
M.Wt | 914.18 |
Cas No. | 53123-88-9 |
Formula | C51H79NO13 |
Synonyms | Sirolimus,(-)-Rapamycin, AY-22989, WY-090217, Antibiotic AY22989 |
Solubility | ≥45.7 mg/mL in DMSO; insoluble in H2O; ≥58.9 mg/mL in EtOH with ultrasonic |
SDF | Download SDF |
Canonical SMILES | O[C@H]1[C@H](OC)C[C@H](C[C@@H](C)[C@H](CC([C@H](C)/C=C(C)/[C@H]([C@@H](OC)C([C@@H](C[C@@H](/C=C/C=C/C=C(C)/[C@@H](OC)C[C@@H]2CC[C@@H](C)[C@@](C(C(N3[C@H]4CCCC3)=O)=O)(O)O2)C)C)=O)O)=O)OC4=O)CC1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
肝细胞生长因子(HGF)诱导的晶状体上皮细胞(LECs) |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应时间 |
10 ng/ml;72 h |
应用 |
在细胞增殖、细胞活力和流式细胞凋亡实验中,在HGF诱导的LECs中,rapamycin不仅有效地抑制细胞增值,而且以剂量依赖的方式诱导细胞凋亡。用siRNA转染进一步研究其潜在的机制,rapamycin通过抑制HGF诱导的AKT/mTOR、ERK和JAK2/STAT3信号分子的磷酸化,从而促进LECs凋亡。而且,AKT、ERK和STAT3的强制表达可以显著抑制rapamycin诱导的细胞凋亡。 |
动物实验[1]: | |
动物模型 |
Ndufs4(?/?) 小鼠 |
剂量 |
8 mg/kg,每隔一天,腹腔注射 |
应用 |
Rapamycin是mTOR信号通路的特异性抑制剂。在Leigh综合征小鼠模型中,rapamycin可以增加存活,并减弱疾病的发展。在缺乏线粒体呼吸链亚基Ndufs4 [NADH脱氢酶(泛醌)Fe-S蛋白4]的小鼠中,rapamycin延迟神经症状的发作,减少神经炎症,并防止脑病变。尽管其精确机制还有待进一步研究,rapamycin诱导代谢转向氨基酸分解代谢,远离糖酵解,减少糖酵解中间体的累积。这种治疗策略可能对各种线粒体疾病有效。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: 1. Tian F, Dong L, Zhou Y et al. Rapamycin-Induced Apoptosis in HGF-Stimulated Lens Epithelial Cells by AKT/mTOR, ERK and JAK2/STAT3 Pathways. Int J Mol Sci. 2014 Aug 11;15(8):13833-48. 2. Johnson SC1, Yanos ME, Kayser EB et al. mTOR inhibition alleviates mitochondrial disease in a mouse model of Leigh syndrome. Science. 2013 Dec 20;342(6165):1524-8. |
描述 | Rapamycin (Sirolimus, AY-22989, WY-090217)是一种特异性的mTOR抑制剂,IC50值约为0.1 nM。 | |||||
靶点 | mTOR | |||||
IC50 | ~0.1 nM |
质量控制和MSDS
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