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Submit ReviewKU 0063794
说明： Selective mTOR inhibitor
化学名： rel-5-[2-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
纯度： ≥97% (HPLC)
生物活性 for KU 0063794
KU 0063794 is a selective inhibitor of mammalian target of rapamycin (mTOR) (IC50 ~10 nM for mTORC1 and mTORC2). Displays no activity at PI 3-kinase or 76 other kinases tested. Inhibits activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK. Suppresses cell growth and induces G1 cell cycle arrest in vitro.
技术数据 for KU 0063794
| 分子量 | 465.54 |
| 公式 | C25H31N5O4 |
| 储存 | Store at RT |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 938440-64-3 |
| PubChem ID | 16736978 |
| InChI Key | RFSMUFRPPYDYRD-CALCHBBNSA-N |
| Smiles | OCC1=C(OC)C=CC(C3=NC2=NC(N5C[C@@H](C)O[C@@H](C)C5)=NC(N4CCOCC4)=C2C=C3)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for KU 0063794
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 4.66 | 10 |
制备储备液 for KU 0063794
以下数据基于产品分子量 465.54。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 21.48 mL | 107.4 mL | 214.8 mL |
| 0.5 mM | 4.3 mL | 21.48 mL | 42.96 mL |
| 1 mM | 2.15 mL | 10.74 mL | 21.48 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
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产品说明书 for KU 0063794
参考文献 for KU 0063794
参考文献是支持产品生物活性的出版物。
Garcia-Martinez et al (2009) Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR). Biochem.J. 421 29 PMID: 19402821
If you know of a relevant reference for KU 0063794, please let us know.
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关键词: KU 0063794, KU 0063794 supplier, KU0063794, mammalian, target, of, rapamycin, inhibitors, inhibits, selective, mTOR, kinases, suppresses, cell, growth, 3725, Tocris Bioscience
14 篇 KU 0063794 的引用文献
引用文献是使用了 Tocris 产品的出版物。 KU 0063794 的部分引用包括：
Hukelmann et al (2016) The cytotoxic T cell proteome and its shaping by the kinase mTOR. J Biol Chem 17 104 PMID: 26551880
Ignacio et al (2020) CDK8 Fine-Tunes IL-6 Transcriptional Activities by Limiting STAT3 Resident Time at the Gene Loci. Cell Rep 33 108545 PMID: 33357429
Xing et al (2018) The 3-Phosphoinositide-Dependent Protein Kinase 1 Inhibits Rod Photoreceptor Development. Front Cell Dev Biol 6 134 PMID: 30364083
Bodur et al (2018) The IKK-related kinase TBK1 activates mTORC1 directly in response to growth factors and innate immune agonists. EMBO J 37 19 PMID: 29150432
López-Cotarelo et al (2015) A novel MEK-ERK-AMPK signaling axis controls chemokine receptor CCR7-dependent survival in human mature dendritic cells. Proc Natl Acad Sci U S A 290 827 PMID: 25425646
Munson et al (2015) mTOR activates the VPS34-UVRAG complex to regulate autolysosomal tubulation and cell survival. Nat Immunol 34 2272 PMID: 26139536
Fei et al (2013) Targeting mTOR to overcome epidermal growth factor receptor tyrosine kinase inhibitor resistance in non-small cell lung cancer cells. PLoS One 8 e69104 PMID: 23874880
Sengupta et al (2013) Regulation of OSR1 and the sodium, potassium, two chloride cotransporter by convergent signals. Free Radic Biol Med 110 18826 PMID: 24191005
Ian E et al (2021) The innate immune kinase TBK1 directly increases mTORC2 activity and downstream signaling to Akt. J Biol Chem 297 100942 PMID: 34245780
Wang et al (2014) SynGAP regulates protein synthesis and homeostatic synaptic plasticity in developing cortical networks. PLoS One 8 e83941 PMID: 24391850
Montané and Menand (2013) ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change. EMBO J 64 4361 PMID: 23963679
Lei et al (2017) SYK kinase mediates brown fat differentiation and activation. Nat Commun 8 2115 PMID: 29235464
Gandin et al (2016) mTORC1 and CK2 coordinate ternary and eIF4F complex assembly. Nat Commun 7 11127 PMID: 27040916
Ling et al (2016) Insulin promotes proliferation and fibrosing responses in activated pancreatic stellate cells. Am J Physiol Gastrointest Liver Physiol 311 G675-G687 PMID: 27609771
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Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
Pathways for KU 0063794
