4E1RCAT

IC50: ∼4 μM (eIF4E/eIF4G)

4E1RCat is an inhibitor of eIF4E:eIF4GI interaction, with an IC ₅₀ an of ∼4 μM. 4E1RCat binding to eIF4E also interferes with eIF4G and 4E-BP binding. 4E1RCat inhibits ribosome recruitment to mRNA in a cap-dependent manner. 4E1RCat blocks the capped mRNA translation, and the translation is activated by CDK1/CYCB1. Nearly all new protein synthesis in both mitosis and interphase is cap-dependent and -sensitive to 4E1RCat treatment, in HeLa and U2OS cells.

4E1RCat (15 mg/kg, i.p.) affacts chemosensitivity of Pten ^+/- Eμ-Myc tumors in mice. 4E1RCat (15 mg/kg, i.p.) sensitizes Pten ^+/- Eμ-Myc and Tsc2 ^+/- Eμ-Myc lymphomas to the cytotoxic effects of doxorubicin (Dxr), and 4E1RCat targets translation in mice.