4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol

Description

GSK690693 is an ATP-competitive, pan-Akt kinase inhibitor with IC₅₀ values of 2, 13, and 9 nM for Akt1, 2, and 3, respectively. It also inhibits other members of the AGC kinase family, including AMPK, DAPK3, PAKs, PKA, PKC, PKG, and PrkX (IC₅₀ values range from 2-81 nM). By preventing the phosphorylation of downstream Akt substrates, GSK690693 has been shown to inhibit proliferation and to induce apoptosis in various human tumor cells in vitro and in xenografts in immunocompromised mice.

Uses

GSK690693 is a pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 2 nM, 13 nM, and 9 nM, respectively

Uses

GSK690693 has been used in western blotting and immunoprecipitations.

Definition

ChEBI: A member of the class of imidazopyridines that is 4-(1-ethylimidazo[4,5-c]pyridin-4-yl)-2-methylbut-3-yn-2-ol carrying additional 2-(4-amino-1,2,5-oxadiazol-3-yl and [(3S)-piperidin-3-yl]methoxy substituents at positions 4 and 7 respectively.

Biochem/physiol Actions

GSK690693 is an ATP competitive, potent pan-AKT kinase inhibitor with IC50 values of 2, 13, and 9 nM against AKT1, 2, and 3, respectively.

storage

Store at -20°C

References

1) Rhodes et al. (2008), Characterization of an Akt kinase inhibitor with potent pharmacodynamics and antitumor activity; Cancer Res., 68 2366 2) Crouthamel et al. (2009), Mechanism and management of AKT inhibitor-induced hyperglycemia; Clin. Cancer Res., 15 217