FIGURE 2.

Dose- and activation state-dependent inhibition of IR/IGF-1R. A, in vitro dose-response measurements of inhibition of IR and IGF-1R catalytic activity by Irfin1 and FR180204. Remaining kinase activity is shown relative to solvent controls. Each data point represents the mean of three replicate measurements. Error bars indicate S.D. B, left: Irfin1 inhibition of activation intermediates of IR. Unphosphorylated (0p), mono (1p)-, di (2p)-, and tri (3p)-phosphorylated forms of IR were purified and subjected to in vitro kinase reactions in the presence of 2, 10, and 100 μm Irfin1. Right: FR180204 inhibition of activation intermediates of IR. Measurements were performed as on the left.