4E1rcat( eIF4E/eIF4G Interaction Inhibitor II )

Catalog No. M14080 CAS No. 328998-25-0

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Product Name

4E1rcat
Note

Research use only, not for human use.
Brief Description

4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E with IC50 of 3.2 μM.
Description

4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E with IC50 of 3.2 μM.
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. 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

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.
Synonyms

eIF4E/eIF4G Interaction Inhibitor II
Pathway

Apoptosis
Target

PERK
Recptor

eIF-4E| eIF-4G
Research Area

Cancer
Indication

——

CAS Number

328998-25-0
Formula Weight

478.45
Molecular Formula

C28H18N2O6
Purity

>98% (HPLC)
Solubility

DMSO: 96 mg/mL (200.64 mM)
SMILES

O=C1/C(C=C(C2=CC=CC=C2)N1C3=CC=C(C(O)=O)C=C3)=C\C4=CC=C(C5=CC=C([N+]([O-])=O)C=C5)O4
Chemical Name

(Z)-4-(3-((5-(4-nitrophenyl)furan-2-yl)methylene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic acid

1.Shuda M, et al. Proc Natl Acad Sci U S A. 2015 May 12;112(19):5875-82.

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