GSK 2334470

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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)
Citations (9)

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 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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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 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:

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

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

Do you know of a great paper that uses GSK 2334470 from Tocris? Please let us know.

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