GSK 2334470

Pricing Availability   Qty
说明: Highly potent, selective PDPK1 (PDK1) inhibitor
化学名: (3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
纯度: ≥98% (HPLC)
说明书
引用文献 (9)
评论

生物活性 for GSK 2334470

GSK 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.

许可信息

Sold for research purposes only under agreement from GlaxoSmithKline

External Portal Information for GSK 2334470

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.

化合物库 for GSK 2334470

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。

技术数据 for GSK 2334470

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.

溶解性数据 for GSK 2334470

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 46.26 100
ethanol 46.26 100

制备储备液 for GSK 2334470

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.

选择批次从而根据批次分子量重新计算:
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

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参考文献 for GSK 2334470

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

9 篇 GSK 2334470 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GSK 2334470 的部分引用包括:

Xing et al (2018) The 3-Phosphoinositide-Dependent Protein Kinase 1 Inhibits Rod Photoreceptor Development. Front Cell Dev Biol 6 134 PMID: 30364083

Busada et al (2015) Retinoic acid regulates Kit translation during spermatogonial differentiation in the mouse. Oncotarget 397 140 PMID: 25446031

Guang et al (2021) Akt phosphorylates insulin receptor substrate to limit PI3K-mediated PIP3 synthesis. Elife 10 PMID: 34253290

Qi et al (2015) PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells. Cancer Cell Int 15 91 PMID: 26421002


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