4E1rcat

SKU: orb1225297

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.

Key Properties

• CAS Number: 328998-25-0
• MW: 478.45
• Purity: >98% (HPLC)
• Formula: C₂₈H₁₈N₂O₆
• 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
• Target: PERK
• Solubility: DMSO: 96 mg/mL (200.64 mM)

Bioactivity

• 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.
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• 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

eIF4E/eIF4G Interaction Inhibitor II

Quick Database Links

Gene Symbol

PERK