Figure 4.

Compound 1 binds KIX and inhibits CREB-mediated gene transcription. A) Compound 1 binds His₆KIX. Different concentrations of His₆KIX were immobilized on Ni–Sepharose beads and incubated with either 1 (□) or 2 (■; 50 μm). The fraction of unbound compounds was analyzed by HPLC. B) Compound 1 inhibits CREB-mediated gene transcription in HEK293T cells. CRE-RLuc-transfected HEK293T cells were treated with increasing concentrations of 1 (□) or 2 (■). The Renilla luciferase activity was measured 4.5 h after forskolin stimulation.