K2605113计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
概述
雷帕霉素是从 吸水链霉菌中分离得到的一种抗真菌抗生素。这种抗生素对所有的 白色念珠菌都有效。它可阻断激活T辅助细胞所需的信号转导通路。Rapamycin 是一种特异性的 mTOR 抑制剂，IC50 为 0.1 nM。
Information
In vitro
Rapamycin inhibits endogenous mTOR activity in HEK293 cells with IC50 of ~0.1 nM, more potently than iRap and AP21967 with IC50 of ~5 nM and ~10 nM, respectively. In Saccharomyces cerevisiae, Rapamycin treatment induces a severe G1/S cell cycle arrest and inhibition of translation initiation to levels below 20% of control. Rapamycin significantly inhibits the cell viability of T98G and U87-MG in a dose-dependent manner with IC50 of 2 nM and 1 μM, respectively, while displaying little activity against U373-MG cells with IC50 of >25 μM despite the similar extent of the inhibition of mTOR signaling. Rapamycin (100 nM) induces G1 arrest and autophagy but not apoptosis in Rapamycin-sensitive U87-MG and T98G cells by inhibiting the function of mTOR.
In vivo
Treatment with Rapamycin in vivo specifically blocks targets known to be downstream of mTOR such as the phosphorylation and activation of p70S6K and the release of inhibition of eIF4E by PHAS-1/4E-BP1, leading to complete blockage of the hypertrophic increases in plantaris muscle weight and fibre size. Short-term Rapamycin treatment, even at the lowest dose of 0.16 mg/kg, produces profound inhibition of p70S6K activity, which correlates with increased tumor cell death and necrosis of the Eker renal tumors. Rapamycin inhibits metastatic tumor growth and angiogenesis in CT-26 xenograft models by reducing the production of VEGF and blockage of VEGF-induced endothelial cell signaling. Rapamycin treatment at 4 mg/kg/day significantly reduces tumor growth of C6 xenografts, and tumor vascular permeability.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~25 μM
Incubation Time：72 hours
Powder Purity:≥99%
规格
英文别名
Rapamune, Sirolimus, NSC-2260804
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Rapamycin (AY-22989)
生化机理
雷帕霉素（AY-22989、Rapamune、Sirolimus、NSC-2260804）是一种特异性 mTOR 抑制剂，在 HEK293 细胞中的 IC50 值约为 0.1 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
610-965-5
分子类型
小分子
Isomeric SMILES
C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)O)C)/C)O)OC)C)C)/C)OC
分子量
914.19
Reaxy-Rn
5848501
高级数据
关联靶点（人）
FKBP1A
Tclin
肽基脯氨酰顺反异构酶 FKBP1A(Peptidyl-prolyl cis-trans isomerase FKBP1A)
(10 活性数据)
FKBP1B
Tchem
肽基脯氨酰顺反异构酶 FKBP1B(Peptidyl-prolyl cis-trans isomerase FKBP1B)
(1 活性数据)
FKBP5
Tchem
肽基脯氨酰顺反异构酶 FKBP5(Peptidyl-prolyl cis-trans isomerase FKBP5)
(1 活性数据)
EIF4E
Tchem
真核翻译起始因子4E(Eukaryotic translation initiation factor 4E)
(1 活性数据)
PDCD4
Tchem
程序性细胞死亡蛋白 4(Programmed cell death protein 4)
(1 活性数据)
MTOR
Tclin
丝氨酸/苏氨酸蛋白激酶 mTOR(Serine/threonine-protein kinase mTOR)
(7 活性数据)
化学和物理性质
比旋光度
-150° (C=0.2,MeOH)
熔点
177 °C(dec.)
安全和危险性（GHS）
象形图
信号词
危险
危险声明
H351: 怀疑会致癌
H372: 长期或反复接触会对器官造成损害
H361: 怀疑破坏生育力或未出生的孩子
预防措施声明
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P405: 密闭存放
P501: 将内容物/容器送到批准的废物处理厂处理
P264: 处理后要彻底洗手。
P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P203: 使用前，获取、阅读并遵守所有安全说明。
P318: 如果暴露或担心，请就医。
P319: 如果你感到不适，请寻求医疗帮助。
RTECS
VE6250000
Merck Index
8114
质检证书(CoA,COO,BSE/TSE 和分析图谱)
技术文档和文章
Small-Molecule Inhibitors: A Practical Guide for Research Selection — A Minimal Evidence Chain and Scenario-Based Validation Framework (Including a Selection Matrix, Case Cards, and Product Tables 1–4)
目录： 技术文章
Functional System Overview of Cellular Metabolic Enzymes in Energy Metabolism, Redox, and Signal Transduction
目录： 技术文章
Central–Peripheral Signaling Networks Regulated by Neuropeptides and the Integration of Energy Metabolism
目录： 技术文章
铁死亡与免疫代谢互作的分子基础
目录： 技术文章
自噬信号通路与选择性自噬研究
目录： 技术文章
Applications of Endocrinology/Hormones in Metabolic Regulation, Reproductive Function, and Disease Research
目录： 技术文章
Role of the HER3 Signaling Network in Tumor Progression, Therapeutic Resistance, and Targeted Intervention
目录： 技术文章
From Metabolic Flux to Protein Degradation: How Metabolic Enzymes and Protein Degradation Systems Jointly Regulate Cell Fate
目录： 技术文章
Molecular Classification, Oncogenic Drivers, and Resistance Mechanisms of Non-Small Cell Lung Cancer
目录： 技术文章
Regulatory Mechanisms of Aging-Related Nutrient Sensing, Inflammation, and Homeostatic Signaling Pathways
目录： 技术文章
天然产物调控脂肪褐变的分子机制
目录： 技术文章
AUTAC or AUTOTAC? Mechanistic Differences Between First- and Second-Generation Autophagy-Targeting Degradation Technologies
目录： 技术文章
Polarity Exposure and Passive Membrane Permeability of bRo5 Molecules: TPSA, EPSA, ETR, and Molecular Chameleonicity
目录： 技术文章
此产品的引用文献
溶液计算器
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危险品化学品经营许可证（带存储）