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4E1rcat

Catalog No. T1742   CAS 328998-25-0

4E1RCat is a dual inhibitor of eIF4E:eIF4 g and eIF4E:4E-BP1 interaction. And it inhibits the binding of eIF4 g to eIF4E with IC50 of 3.2 μM.

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4E1rcat Chemical Structure
4E1rcat, CAS 328998-25-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 47.00
5 mg In stock $ 68.00
10 mg In stock $ 93.00
25 mg In stock $ 165.00
50 mg In stock $ 207.00
100 mg In stock $ 369.00
1 mL * 10 mM (in DMSO) In stock $ 75.00
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Purity: 99.36%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 4E1RCat is a dual inhibitor of eIF4E:eIF4 g and eIF4E:4E-BP1 interaction. And it inhibits the binding of eIF4 g to eIF4E with IC50 of 3.2 μM.
Targets&IC50 eIF4 g:3.2 μM
Kinase Assay Kinase Assay: GSK3 scintillation proximity assay is done. The competition experiments are carried out in duplicate with 10 concentrations of the inhibitor in clear-bottomed microtiter plates. The biotinylated peptide substrate biotin-AAEELDSRAGS(PO3H2)PQL, is added at a final concentration of 2 μM in an assay buffer containing 6 milliunits of recombinant human GSK3 (equal mix of both α and β), 12 mM MOPS, pH 7.0, 0.3 mM EDTA, 0.01% β-mercaptoethanol, 0.004% Brij 35, 0.5% glycerol, and 0.5 μg of bovine serum albumin/25 μl and preincubated for 10–15 min. The reaction is initiated by the addition of 0.04 μCi of [γ-33P]ATP and unlabeled ATP in 50 mM Mg(Ac)2 to a final concentration of 1 μM ATP and assay volume of 25 μl. Blank controls without peptide substrate are used. After incubation for 20 min at room temperature, each reaction is terminated by the addition of 25 μl of stop solution containing 5 mM EDTA, 50 μM ATP, 0.1% Triton X-100, and 0.25 mg of streptavidin-coated SPA beads corresponding to 35 pmol of binding capacity. After 6 h the radioactivity is determined in a liquid scintillation counter.
Molecular Weight 478.45
Formula C28H18N2O6
CAS No. 328998-25-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 23.9 mg/mL (50 mM)

TargetMolReferences and Literature

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

TargetMolCitations

1. Chen C, Zhang X, Wang Y, et al. Translational and Post-translational Control of Human Naïve versus Primed Pluripotency. iScience. 2021: 103645. 2. Xiang H, Zhou M, Li Y, et al.Drug discovery by targeting the protein‒protein interactions involved in autophagy.Acta Pharmaceutica Sinica B.2023 3. Xiang H, Liu R, Zhang X, et al.Discovery of Small-Molecule Autophagy Inhibitors by Disrupting the Protein–Protein Interactions Involving Autophagy-Related 5.Journal of Medicinal Chemistry.2023

Related compound libraries

This product is contained In the following compound libraries:
Reprogramming Compound Library Apoptosis Compound Library Endoplasmic Reticulum Stress Compound Library Bioactive Compound Library Inhibitor Library Autophagy Compound Library Anti-Aging Compound Library Bioactive Compounds Library Max HIF-1 Signaling Pathway Compound Library PPI Inhibitor Library

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Keywords

4E1rcat 328998-25-0 Apoptosis Autophagy PERK inhibit Inhibitor 4E-1rcat Eukaryotic Initiation Factor (eIF) inhibitor

 

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