GSK 2334470

Pricing Availability   Qty
Cat.No. 4143 - GSK 2334470 | C25H34N8O | CAS No. 1227911-45-6
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)
Datasheet
Citations (5)
Reviews
Literature (1)

Biological Activity

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

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

GSK 2334470 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.26 100
ethanol 46.26 100

Preparing Stock Solutions

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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References

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.

View Related Products by Product Action

View all Phosphoinositide-dependent Kinase 1 Inhibitors

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

5 Citations for GSK 2334470

Citations are publications that use Tocris products. Selected citations for GSK 2334470 include:

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

Heberle et al (2019) The PI3K and MAPK/p38 pathways control stress granule assembly in a hierarchical manner. Life Sci Alliance 2 PMID: 30923191

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

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

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


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Literature in this Area

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases