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GSK2334470

Chemical Structure : GSK2334470

CAS No.: 1227911-45-6

GSK2334470 (GSK 2334470)

Catalog No.: PC-49261Not For Human Use, Lab Use Only.

GSK2334470 (GSK 2334470) is a potent, highly specific inhibitor of PDK1 with IC50 of 10 nM, does not inhibit 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 5 uM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK2334470 (GSK 2334470) is a potent, highly specific inhibitor of PDK1 with IC50 of 10 nM, does not inhibit 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 5 uM.
GSK2334470 ablated T-loop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF1 (insulin-like growth factor 1) in HEK-293, U87 or MEF (mouse embryonic fibroblast) cells, GSK2334470 also inhibited T-loop phosphorylation and activation of Akt.
GSK2334470 inhibited activation of an Akt1 mutant lacking the PH domain (pleckstrin homology domain) more potently than full-length Akt1.
GSK2334470 also suppressed T-loop phosphorylation and activation of RSK2 (p90 ribosomal S6 kinase 2), another PDK1 target activated by the ERK (extracellular-signal-regulated kinase) pathway.

Physicochemical Properties

M.Wt 462.602
Formula C25H34N8O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide

References

1. Najafov A, et al. Biochem J. 2011 Jan 15;433(2):357-69.

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