Chemical Name: (3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide. Alternate Names: GSK-470
Potent and selective PDK1 inhibitor
Molekulargewicht:
462.60
Reinheit:
>98% by HPLC NMR (Conforms)
Formulierung:
Off-white solid
CAS Nummer:
[1227911-45-6]
Formel:
C25H34N8O
Anwendungsbeschreibung:
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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