Calbiochem Eif2-Gtp-Trnaimet Ternary Complex Inhibitor, Btdcpu, The Eif2-Gtp-Trna, Each

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A cell-permeable n, n'-diarylurea that acts as an inhibitor of the formation of the ternary complex of eukaryotic translation initiation factor 2 (eif2), gtp and the initiator methionine trna (met-trnai), a key regulatory step of translation initiation. It directly activates heme-regulated inhibitor kinase (hri), which then phosphorylates eif2α in cells at 10μm and in cell-free extracts dose-dependently, and thereby prevents respective ternary complex formation without elevating oxidative stress. The sensitivities of various cancer cell lines to the anti-proliferative effects of this compound are shown to correlate with the expression of hri. Furthermore, this compound displays tumor growth inhibition in a mice xenograft model of mcf-7 human breast cancer cells at 175mg/kg, in vivo .