Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092
Fig 1
Determination of Kd values for the allosteric inhibitors ARQ 092, ARQ 751, and MK-2206 and pathway inhibition by ARQ 092 and ARQ 751 in transfected 293T cells.
(A) The Kd values of ARQ 092, ARQ 751, and MK-2206 were determined against AKT-WT and AKT1-E17K. (B) 293T cells were transiently transfected with pcDNA-E17K-GFP and then treated with various concentrations of ARQ 092 or ARQ 751 for 2 hours. pAKT(S473) and total AKT were assessed. Densitometry analysis was performed and relative pAKT(S473) level was shown as percentage (%) of pAKT/total AKT.