Catalog Number: 4143
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Additional Information
Licensing Caveats:
Sold for research purposes only under agreement from GlaxoSmithKline
Background References
  1. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1.
    Najafov et al.
    Biochem.J., 2011;433:357
  2. Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of BrafV600E::Pten(-/-) melanoma.
    Scortegagna et al.
    Oncogene, 2014;33:4330

The citations listed below are publications that use Tocris products. Selected citations for GSK 2334470 include:

Showing Results 1 - 3 of 3

  1. Retinoic acid regulates Kit translation during spermatogonial differentiation in the mouse.
    Authors: Busada Et al.
  2. PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells.
    Authors: Qi Et al.
    Cancer Cell Int
  3. Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer.
    Authors: Al-Ejeh Et al.
    PLoS One
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