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
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Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1.
Najafov et al.
Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of BrafV600E::Pten(-/-) melanoma.
Scortegagna et al.
The citations listed below are publications that use Tocris products. Selected citations for GSK 2334470 include:
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