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Submit ReviewGSK 2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDPK1) inhibitor (IC50 ~ 10 nM). Exhibits no effect on other kinases including Aurora, ROCK, p38 MAPK and PI 3-K. Suppresses T-loop phosphorylation and subsequent activation of PDK1 substrates S6K1, SGK and RSK in vitro; exhibits limited inhibitory effect on Akt activation. Delays melanomagenesis and metastasis in BrafV600E::Pten(-/-) mice.
Sold for research purposes only under agreement from GlaxoSmithKline
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK 2334470 is reviewed on the chemical probes website.
GSK 2334470 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 462.59 |
公式 | C25H34N8O |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1227911-45-6 |
PubChem ID | 46215815 |
InChI Key | QLPHOXTXAKOFMU-WBVHZDCISA-N |
Smiles | C[C@H]1N(C3=NC(NC)=NC(C4=CC(NN=C5N)=C5C=C4)=C3)C[C@@H]([C@](NC2CCCCC2)=O)CC1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 46.26 | 100 | |
ethanol | 46.26 | 100 |
以下数据基于产品分子量 462.59。 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 |
---|---|---|---|
1 mM | 2.16 mL | 10.81 mL | 21.62 mL |
5 mM | 0.43 mL | 2.16 mL | 4.32 mL |
10 mM | 0.22 mL | 1.08 mL | 2.16 mL |
50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
参考文献是支持产品生物活性的出版物。
Najafov et al (2011) Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem.J. 433 357 PMID: 21087210
Scortegagna et al (2014) Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of BrafV600E::Pten(-/-) melanoma. Oncogene 33 4330 PMID: 24037523
If you know of a relevant reference for GSK 2334470, please let us know.
关键词: GSK 2334470, GSK 2334470 supplier, GSK2334470, PDK1, S6K, p70, ribosomal, SGK, serum, glucocorticoid, protein, kinases, inhibits, inhibitors, Akt, 3-phosphoinositide-dependent, selective, PDPK1, Phosphoinositide-dependent, Kinase, 1, 4143, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GSK 2334470 的部分引用包括:
Guang et al (2021) Akt phosphorylates insulin receptor substrate to limit PI3K-mediated PIP3 synthesis. Elife 10 PMID: 34253290
Raymond A et al (2014) Activation of 3-phosphoinositide-dependent kinase 1 (PDK1) and serum- and glucocorticoid-induced protein kinase 1 (SGK1) by short-chain sphingolipid C4-ceramide rescues the trafficking defect of δF508-cystic fibrosis transmembrane conductance regulat J Biol Chem 289 35953-68 PMID: 25384981
Heberle et al (2019) The PI3K and MAPK/p38 pathways control stress granule assembly in a hierarchical manner. Life Sci Alliance 2 PMID: 30923191
Al-Ejeh et al (2014) Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer. PLoS One 5 3145 PMID: 24762669
Busada et al (2015) Retinoic acid regulates Kit translation during spermatogonial differentiation in the mouse. Oncotarget 397 140 PMID: 25446031
Richard A et al (2020) Inhibition of class I PI3K enhances chaperone-mediated autophagy. J Cell Biol 219 PMID: 33048163
Natalia et al (2016) The hVps34-SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth. EMBO J 35 1902-22 PMID: 27481935
Qi et al (2015) PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells. Cancer Cell Int 15 91 PMID: 26421002
Xing et al (2018) The 3-Phosphoinositide-Dependent Protein Kinase 1 Inhibits Rod Photoreceptor Development. Front Cell Dev Biol 6 134 PMID: 30364083
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