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CCT020312 is an activator of eukaryotic translation initiation factor 2α kinase 3 (EIF2AK3).1 It increases phosphorylation of eIF2α at serine 51 in HT-29 colon carcinoma and MCF-7 breast cancer cells when used at a concentration of 10 µM, an effect not seen in cells transfected with EIF2AK3 siRNA. It reduces phosphorylation of the tumor suppressor retinoblastoma (Rb) protein in HT-29 cells (EC50 = 5.1 µM). CCT020312 (10 µM) rapidly reduces the level of cyclin D1 in HT-29 cells. It also inhibits the growth of HT-29 cells (GI50 = 2.1 µM).
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1. Mechanism-