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Submit ReviewGSK 2334470
Description: Highly potent, selective PDPK1 (PDK1) inhibitor
Chemical Name: (3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
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.
Compound Libraries for GSK 2334470
GSK 2334470 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for GSK 2334470
| M. Wt | 462.59 |
| Formula | C25H34N8O |
| Storage | Store at +4°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GSK 2334470
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.26 | 100 | |
| ethanol | 46.26 | 100 |
Preparing Stock Solutions for GSK 2334470
The following data is based on the product molecular weight 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.
| Concentration / Solvent Volume / Mass | 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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Product Datasheets for GSK 2334470
References for GSK 2334470
References are publications that support the biological activity of the product.
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.
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Keywords: 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 Citations for GSK 2334470
Citations are publications that use Tocris products. Selected citations for GSK 2334470 include:
Richard A et al (2020) Inhibition of class I PI3K enhances chaperone-mediated autophagy. J Cell Biol 219 PMID: 33048163
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
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
Heberle et al (2019) The PI3K and MAPK/p38 pathways control stress granule assembly in a hierarchical manner. Life Sci Alliance 2 PMID: 30923191
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
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
Do you know of a great paper that uses GSK 2334470 from Tocris? Please let us know.
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