GSK 2334470

Cat. No. 4143

GSK 2334470 C25H34N8O [1227911-45-6]

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Special Conditions

No more than 500 mg per individual per year to be sold without prior permission from the licence holder.

Chemical Name: (3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide

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.

Technical Data

M.Wt:
462.59
Formula:
C25H34N8O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1227911-45-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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.

Najafov et al (2011) Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem.J. 433 357. PMID: 21087210.

If you know of a relevant reference for this product please let us know.

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

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

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

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? If so please let us know.

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Keywords: GSK 2334470, supplier, GSK2334470, PDK1, S6K, p70, ribosomal, SGK, serum, glucocorticoid, protein, kinases, inhibits, inhibitors, Akt, 3-phosphoinositide-dependent, selective, PDPK1, Tocris Bioscience, Phosphoinositide-dependent Kinase 1 Inhibitor products

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