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4EGI-1

In stock
Catalog No.
B3696
Competitive eIF4E/eIF4G interaction inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$130.00
In stock
10mg
$137.00
In stock
25mg
$235.00
In stock

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Email: [email protected]

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4EGI-1 is a small-molecule inhibitor of eIF4E/eIF4G interaction with IC50 value of 125μM [1].

The eIF4E/eIF4G complex plays a key role in gene translation initiation and is regulated by 4E-BP. Overexpression of eIF4E or eIF4G can induce malignant transformation in mammalian cells. As a mimic peptide of 4E-BP, 4EGI-1 competes with eIF4G and disrupts the association of eIF4E/eIF4G. The KD value for 4EGI-1 binding to eIF4E is 25μM. 4EGI-1 can not affect the binding of 4E-BP to eIF4E and instead causes increase of this binding level. In addition, 4EGI-1 is found to inhibit the Cap-dependent translation while enhances the initiation factor-independent translation. In Jurkat leukemia T cells, 4EGI-1 also causes eIF4G to be displaced from eIF4E [1].

References:
[1] Moerke N J, Aktas H, Chen H, et al. Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. Cell, 2007, 128(2): 257-267.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt451.28
Cas No.315706-13-9
FormulaC18H12Cl2N4O4S
Solubility≥22.56mg/mL in DMSO
SDFDownload SDF
Canonical SMILESC1=CC=C(C(=C1)CC(=NNC2=NC(=CS2)C3=CC(=C(C=C3)Cl)Cl)C(=O)O)[N+](=O)[O-]
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Protocol

Cell experiment [1]:

Cell lines

Jurkat cells

Preparation method

The solubility of this compound in DMSO is > 22.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0 ~ 200 μM; 24 hrs

Applications

In Jurkat cells, 4EGI-1 (> 50 μM) treatment induced cell death after 24 hrs. In addition, 4EGI-1 significantly increased subG1 DNA content, which was inhibited by cotreatment with the caspase inhibitor zVAD-FMK.

References:

[1]. Moerke N J, Aktas H, Chen H, et al. Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. Cell, 2007, 128(2): 257-267.

Biological Activity

Description 4EGI-1 is a competitive inhibitor of eIF4E/eIF4G interaction by binding to eIF4E with KD of 25 μM.
Targets eIF4E/eIF4G          
IC50 25 μM (KD)          

Quality Control

Chemical structure

4EGI-1

Related Biological Data

4EGI-1

Related Biological Data

4EGI-1