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

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

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10 mM * 1 mL in DMSO
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

eIF4

 

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].

MedChemExpress (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].

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

Molecular Weight

478.45

Formula

C28H18N2O6

CAS No.
Appearance

Solid

Color

Brown to purplish red

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 18.33 mg/mL (38.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo Dissolution Calculator
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Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0901 mL 10.4504 mL 20.9008 mL 52.2521 mL
5 mM 0.4180 mL 2.0901 mL 4.1802 mL 10.4504 mL
10 mM 0.2090 mL 1.0450 mL 2.0901 mL 5.2252 mL
15 mM 0.1393 mL 0.6967 mL 1.3934 mL 3.4835 mL
20 mM 0.1045 mL 0.5225 mL 1.0450 mL 2.6126 mL
25 mM 0.0836 mL 0.4180 mL 0.8360 mL 2.0901 mL
30 mM 0.0697 mL 0.3483 mL 0.6967 mL 1.7417 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
4E1RCat
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HY-14427
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