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Product Category詳細介紹
| 品牌 | absin | 貨號 | abs810030 |
|---|---|---|---|
| 規格 | 5mg | 供貨周期 | 現貨 |
| 主要用途 | 作用于HEK293細胞,抑制內源性mTOR活性 | 應用領域 | 化工,生物產業,農林牧漁,制藥/生物制藥,綜合 |
Rapamycin 53123-88-9
| 產品描述 | |
| 描述 | Rapamycin (Sirolimus)是一種特定的 mTOR 抑制劑，在 HEK293細胞中，IC50 為 ~0.1nM。 |
| 純度 | >98 % |
| 儲存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | 雷帕霉素；Sirolimus；AY 22989；NSC-2260804 |
| 外觀 | Lyophilized powder |
| 可溶性/溶解性 | DMSO ：20 mg/mL (21.87 mM) |
| 生物活性 | |
| 靶點 | mTOR |
| In vitro(體外研究) | 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(體內研究) | 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. |
| 參考文獻 | |
| 參考文獻 | [1] Edwards SR, et al. J Biol Chem, 2007, 282(18), 13395-13401. [2] Barbet NC, et al. Mol Biol Cell, 1996, 7(1), 25-42. [3] Takeuchi H, et al. Cancer Res, 2005, 65(8), 3336-3346. |
| 研究領域 | |
| 研究領域 | CancerCell cycleCell cycle inhibitorsOther CardiovascularHeartCardiogenesisTranscription factors/regulators Cell CycleCell Cycle InhibitorsOther EpigeneticsDNA / RNADNA Damage & RepairDNA Damage ResponseDNA Damage Recognition MetabolismTypes of diseaseObesity NeuroscienceDevelopment NeuroscienceProcesses Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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