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.
External Portal Information
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Soluble to 100 mM in DMSO and to 100 mM in ethanol
Store at +4°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
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Sold for research purposes only under agreement from GlaxoSmithKline
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Note: No more than 500 mg per individual per year to be sold without prior permission from the licence holder.