Fig. 7.

HTS of a 1,200 compound library in the cancer cell-based assay utilizing PC3-MM2 cells. (A) One thousand two hundred compounds from the Prestwick library were screened using a single-point cell-based luciferase refolding drug screen that resulted in two potential hits, ethoxyquin and biperiden. (B) Inhibition of luciferase refolding with ethoxyquin (■), biperiden (▲), and 17-AAG (●) in the rabbit reticulocyte assay. These data are the mean±SEM from two independent experiments performed in duplicate (n=2). (C) The molecular structures of ethoxyquin and biperiden, along with a previous scaffold (compound 9), identified in a rabbit reticulocyte screen by Galam et al.²⁴ (D) Western blots for client protein degradation of cdc25C and AKT in PC3-MM2 cells treated with 17-AAG, 174, ethoxyquin, and biperiden. These results are representative of three independent experiments (n=3).