Torin 1
作者：齊岳
發(fā)布時間：2023-09-11
09:07:28
點擊數(shù)：
產(chǎn)品名稱：Torin 1
產(chǎn)品描述：
| 產(chǎn)品描述 | Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K. |
| 靶點活性 | mTORC2:10 nM, mTORC1:2 nM |
| 體外活性 | Torin1（20 mg/kg）對U87 mg異種移植模型有效的,且可有效抑制和外周組織中的mTOR下游效應(yīng)蛋白. |
| 體內(nèi)活性 | Torin1通過耐雷帕霉素機(jī)制引起細(xì)胞周期阻滯,并且其不依賴于mTORC2。Torin1比雷帕霉素對mTORC1依賴的表現(xiàn)型干擾更完全。在近期的一項研究中表明,Torin1通過活化人內(nèi)分泌細(xì)胞系BON 中MEK/ERK/c-Jun通路,能夠增加神經(jīng)降壓素分泌和基因表達(dá)。Torin1（2、10 nM）可分別抑制mTORC1 和mTORC2底物的磷酸化。 |
| 激酶實驗 | mTORC1 and mTORC2 in Vitro Kinase Assays: To produce soluble mTORC1, HEK-293T cell lines that stably express N-terminally FLAG-tagged Raptor are generated using vesicular stomatitis virus G-pseudotyped MSCV retrovirus. For mTORC2, similar HeLa cells that stably express N-terminally FLAG-tagged Protor-1 are generated. Both complexes are purified by lysing cells in 50 mm HEPES, pH 7.4, 10 mm sodium pyrophosphate, 10 mm sodium β-glycerophosphate, 100 mm NaCl, 2 mm EDTA, 0.3% CHAPS. Cells are lysed at 4 °C for 30 min, and the insoluble fraction is removed by microcentrifugation at 13,000 rpm for 10 min. Supernatants are incubated with FLAG-M2 monoclonal antibody-agarose for 1 h and then washed three times with lysis buffer and once with lysis buffer containing a final concentration of 0.5 M NaCl. Purified mTORC1 is eluted with 100 μg/mL 3×FLAG peptide in 50 mm HEPES, pH 7.4, 100 mm NaCl. Eluate can be aliquoted and stored at -80 °C. Substrates S6K1 and Akt1 are purified. Kinase assays are performed for 20 min at 30 °C in a final volume of 20 μL consisting of the kinase buffer (25 mm HEPES, pH 7.4, 50 mm KCl, 10 mm MgCl2, 500 μm ATP) and 150 ng of inactive S6K1 or Akt1 as substrates. Reactions are stopped by the addition of 80 μL of sample buffer and boiled for 5 min. Samples are subsequently analyzed by SDS-PAGE and immunoblotting. |
| 細(xì)胞實驗 | Cell viability is assessed with the CellTiter-Glo Luminescent Cell Viability Assay. On Day 0, 96-well plates are seeded with 500 cells per well and grown overnight. On Day 1, cells are treated with the appropriate compounds and subsequently analyzed on Days 3-5. For analysis, plates are incubated for 60 min at room temperature; 50 μL of CellTiter-Glo reagent is added to each well, and plates are mixed on an orbital shaker for 12 min. Luminescence is quantified on a standard plate luminometer. (Only for Reference) |
| 分子量 | 607.62 |
| 分子式 | C35H28F3N5O2 |
| CAS No. | 1222998-36-8 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 2.5 mM
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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