Potent (IC50 = 10 nM) and selective inhibitor of 3-Phosphoinositide-dependent kinase 1 (PDK1), which phosphorylates and activates a group of protein kinases in the AGC/PKG/PKC family.1 It is more effective at inhibiting PDK1 substrates that are activated in the cytosol rather than at the plasma membrane.1 GSK2334470 delayed melanogenesis and metastasis in Braf(V600E)::Pten(-/-) mice.2 It also displays antitumor activity against multiple myeloma synergistically with mTORC1/2 inhibitor PP2423 and proteasome inhibitor MG-1324.
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