1. Cell Cycle/DNA Damage
    Autophagy
  2. Eukaryotic Initiation Factor (eIF)
    Autophagy
  3. 4E1RCat

4E1RCat 

Cat. No.: HY-14427 Purity: >98.0%
Handling Instructions

4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC50 an of ∼4 μM.

For research use only. We do not sell to patients.

4E1RCat Chemical Structure

4E1RCat Chemical Structure

CAS No. : 328998-25-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 103 In-stock
Estimated Time of Arrival: December 31
5 mg USD 94 In-stock
Estimated Time of Arrival: December 31
10 mg USD 162 In-stock
Estimated Time of Arrival: December 31
50 mg USD 748 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC50 an of ∼4 μM.

IC50 & Target

IC50: ∼4 μM (eIF4E/eIF4G)[1]

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[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].

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].

Molecular Weight

478.45

Formula

C₂₈H₁₈N₂O₆

CAS No.

328998-25-0

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

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
In Vitro: 

DMSO : 5.4 mg/mL (11.29 mM; Need warming)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

TSC2+/-Eμ-Myc and Eμ-Myc lymphomas are seeded in 96-well plates at 106 cells/mL in the presence of increasing concentrations of doxorubicin (Dxr) (ranging from 3.9 nM to 250 nM) and 4E1RCat (ranging from 78.13 nM to 10 000 nM) at a constant ratio of either 20:1 or 40:1. Twenty four hours later, a MTS assay is performed. To this end, Cell Proliferation Assay is added to the plates and the plates further incubated for up to 3 h, followed by measuring the OD490. Values obtained are standardized against DMSO controls[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
One million secondary Pten+/-Eμ-Myc, Tsc2+/-Eμ-Myc, or Eμ-Myc lymphoma cells are injected into the tail vein of 6-8 week old female C57BL/6 mice. When tumors are palpable, mice are treated with rapamycin (4 mg/kg daily for 5 d), 4E1RCat (15 mg/kg daily for 5 d), or doxorubicin (once at 10 mg/kg). Compounds are administered via intraperitoneal (i.p.) injection in 5.2% PEG 400/ 5.2% Tween 80. For combination studies, rapamycin or 4E1RCat are injected i.p. daily for five consecutive days, with doxorubicin being administered once on day two. Animals are palpated daily to monitor for the onset of tumors. Tumor-free survival is defined as the time between disappearance and reappearance of tumors. Data is analyzed using the log-rank test for statistical significance presented in Kaplan-Meier format[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: >98.0%

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Keywords:

4E1RCatEukaryotic Initiation Factor (eIF)AutophagyInhibitorinhibitorinhibit

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4E1RCat
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