Research Paper Volume 8, Issue 5 pp 958—973
Preclinical validation of a novel compound targeting p70S6 kinase in breast cancer
Figure 1. FS-115 inhibits p70S6K1 activity in vitro. (A) p70S6K1 (B) p70S6K2 and (C) AKT2 were assayed in radiometric ATP-competitive kinase assay, in the presence or absence of increasing concentrations of FS-115 with 10mM Mg and 15μM ATP. The IC50 graph was plotted using XLFit version 5.3 (ID Business Solutions). Sigmoidal dose-response (variable slope) curves are fitted using non-linear regression analysis. The results are presented as the percentage of kinase activity relative to the DMSO-treated control. (D) Selectivity map displaying percentage inhibition of 268 kinases tested in radiometric ATP-competitive kinase assay, using FS-115 at 0.5μM. The extent of inhibition is represented by colored dots according to the scale displayed. Each dot represents the mean percentage inhibition derived from a duplicate experiment.