[CAS NO. 328998-25-0] 4E1RCat
PRODUCTS SPECIFICATIONS [328998-25-0]
DESCRIPTION [328998-25-0]
Overview
| MDL | MFCD01931282 |
|---|---|
| Molecular Weight | 478.45 |
| Molecular Formula | C28H18N2O6 |
| SMILES | O=C(O)C1=CC=C(N2C(/C(C=C2C3=CC=CC=C3)=C\C4=CC=C(C5=CC=C([N+]([O-])=O)C=C5)O4)=O)C=C1 |
2 Publications Citing Use of MCE
Summary
4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC 50 an of ∼4 μM.
IC50 & Target
|
eIF4 |
In Vitro
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 [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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 18.33 mg/mL ( 38.31 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0901 mL | 10.4504 mL | 20.9008 mL |
| 5 mM | 0.4180 mL | 2.0901 mL | 4.1802 mL |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0901 mL |
References
- [1] Cencic R, et al. Reversing chemoresistance by small molecule inhibition of the translation initiation complex eIF4F. Proc Natl Acad Sci U S A. 2011 Jan 18;108(3):1046-51.
- [2] Shuda M, et al. CDK1 substitutes for mTOR kinase to activate mitotic cap-dependent protein translation. Proc Natl Acad Sci U S A. 2015 May 12;112(19):5875-82.