tcsc3172 4E1RCat

4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC₅₀ an of ∼4 μM.

IC50 & Target: IC50: ∼4 μM (eIF4E/eIF4G)^[1]

In Vitro: 4E1RCat is an inhibitor of eIF4E:eIF4GI interaction, with an IC₅₀ 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^[1]. 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^[2].

In Vivo: 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^[1].