GSK 2334470

• Supplier: Tocris Bioscience
• Catalog: 5303
• Prices: $225.00, $925.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 1227911-45-6
• Chemical Name: (3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
• Formula: C25H34N8O
• Molecular Weight: 462.59
• Purity: >98 %
• Description: Potent 3-phosphoinositide-dependent protein kinase (PDPK1) inhibitor (IC 50 ~ 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 Braf V600E ::Pten (-/-) mice.

Product References

Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. - Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1.

Najafov A, Sommer EM, Axten JM, Deyoung MP, Alessi DR. Biochem J. 2011 Jan 15;433(2):357-69.

Genetic inactivation or pharmacological inhibition of Pdk1 delays development and - Genetic inactivation or pharmacological inhibition of Pdk1 delays development and

Scortegagna M, Ruller C, Feng Y, Lazova R, Kluger H, Li JL, De SK, Rickert R, Pellecchia M, Bosenberg M, Ronai ZA. Oncogene. 2014 Aug 21;33(34):4330-9.