Figure 1.

TG003 suppresses kinase activity of CK1 family members in vitro. Recombinant CK1 family members were incubated with the substrate peptide CKtide in the presence of different concentrations of TG003 and IC261. TG003 (open circle) and IC261 (closed square) inhibited CK1 family members in a dose-dependent manner. The IC₅₀ values of TG003 on the kinase activity of CK1α, δ, ϵ, γ1, γ2 and γ3were 0.33, 0.34, 1.4, 1.5, 0.93 and 0.88 μM, respectively. The IC₅₀ values of IC261 were 0.19, 0.60, 0.86, > 30, > 30 and > 30 μM, respectively. Representative dose-response curves with Hill slope are shown. The results are presented as an average of duplicated experiments.