Molecular Formula | C28H18N2O6 |
Molar Mass | 478.45 |
Solubility | DMSO : 18.33 mg/mL (38.31 mM; Need ultrasonic) |
Appearance | powder |
Color | brown to dark brown |
Storage Condition | 2-8°C |
Use | 4E1RCat is a cap-dependent translation inhibitor capable of inhibiting the eIF4E:eIF4GI interaction with an IC50 value of about 4 μM. |
In vitro study | 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. |
In vivo study | 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. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.09 ml | 10.45 ml | 20.901 ml |
5 mM | 0.418 ml | 2.09 ml | 4.18 ml |
10 mM | 0.209 ml | 1.045 ml | 2.09 ml |
5 mM | 0.042 ml | 0.209 ml | 0.418 ml |
biological activity | 4E1RCat is a dual inhibitor of eIF4E: eIF44 G and eIF4E:4E-BP1 interaction, with IC50 of 3.2 μM to inhibit eIF44E. |
target | IC50: 4 μ m (eIF4E/eIF4G) |
in vitro study | 4E1RCat is an inhibitor of eIF4E:eIF4GI interaction, with an IC 50 an of 4 μ M. 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. |
in vivo study | 4 E1RCat (15 mg/kg, I. p.) affacts chemosensitivity of Pten /- Eμ-Myc Tumors in MICE. 4 E1RCat (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. |