324518

eIF4E/eIF4G Interaction Inhibitor II, 4E1RCat

The eIF4E/eIF4G Interaction Inhibitor II, 4E1RCat controls the biological activity of eIF4E/eIF4G interaction. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): eIF4E/eIF4G Interaction Inhibitor II, 4E1RCat, 4-((3 E)-3-((5-(4-Nitrophenyl)furan-2-yl)methylidene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic acid, eIF4F Inhibitor II
• Empirical Formula (Hill Notation): C₂₈H₁₈N₂O₆
• Molecular Weight: 478.45
• UNSPSC Code: 12352200
• NACRES: NA.32

Properties

• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: dark brown
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

A cell-permeable oxopyrrolyl benzoate compound that blocks the assembly of eukaryotic translation initiation factor (eIF) 4F complex (eIF4F) as well as disrupts preformed eIF4F by competing against eIF4G for eIF4E binding. Specifically blocks cap-dependent, but not cap-independent, protein translations in cell-free translation assays and inhibits protein, but not DNA or RNA, synthesis in MDA-MB-231 and HeLa cultures (50 µM) in a reversible manner. Although not effective when administered alone (15 mg/kg, i.p. daily for 5 days), 4E1RCat is shown to significantly prolong Pten^+/-Eµ-myc and Tsc^+/-Eµ-myc, but not Eµ-myc, tumor remission time when combined with Doxorubicin (Cat. No. 324380) treatment (10 mg/kg, i.p. once on day 2) in mice in vivo. Unlike 4EGI-1 (Cat. No. 324517), 4E1RCat also blocks eIF4E and 4E-BP1 interaction.

A cell-permeable oxopyrrolyl benzoate compound that blocks the assembly of eukaryotic translation initiation factor (eIF) 4F complex (eIF4F) as well as disrupts preformed eIF4F by competing against eIF4G for eIF4E binding. Specifically blocks cap-dependent, but not cap-independent, protein translations in cell-free translation assays and inhibits protein, but not DNA or RNA, synthesis in MDA-MB-231 and HeLa cultures (50 µM) in a reversible manner. Although not effective when administered alone (15 mg/kg, i.p. daily for 5 days), 4E1RCat is shown to significantly prolong Pten^+/-Eµ-myc and Tsc^+/-Eµ-myc, but not Eµ-myc, tumor remission time when combined with Doxorubicin (Cat. No. 324380) treatment (10 mg/kg, i.p. once on day 2) in mice in vivo. Unlike 4EGI-1 (Cat. No. 324517), 4E1RCat also blocks eIF4E and 4E-BP1 interaction.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Very fluffy material, not recommended for subdividing solid material by hand-weighing. Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Cencic, R., et al. 2011. Proc. Natl. Acad. Sci. USA108, 1046.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable