ERGi-USU selectively inhibits the growth of ERG-positive VCaP prostate cancer cells, COLO320 colon cancer cells, KG-1 and MOLT-4 leukemia cells with minimal effect on ERG-negative cells or normal prostate or endothelial cells (IC50 = 169 nM for cell growth and 315 nM for ERG protein in VCaP cells). It selectively inhibits the kinase RIOK2 (Kd = 200 nM) causing disruption of ribosomal biogenesis and ribosomal stress.
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