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4E1RCat

In stock
Catalog No.
B3697
Dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$140.00
In stock
5mg
$70.00
In stock
10mg
$110.00
In stock

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4E1RCat is a dual inhibitor of eIF4E:4E-BP1 and eIF4E:eIF4G interaction, and inhibits the binding of eIF4G to eIF4E with IC50 of 3.2 μM.
The complexity of eIF4A, eIF4E and eIF4G together forms the eIF4F, the eukaryotic initiation factor, which stimulates the loading of ribosomes onto mRNA templates in protein synthesis. The inhibition of this cap-dependent translation is associated with cancer initiation and progression [1].
4E1RCat prevents assembly of the eIF4F complex and inhibits cap-dependent translation [1]. 4E1RCat significantly inhibited 5′-cap-mediated mCherry synthesis while had little effect on the IRES-mediated DIAPH1-HA synthesis, which confirmed the specific inhibitory effect of 4E1RCat on 5′-cap-mediated translation [2].
References:
[1]. Cencic R, Hall DR, Robert F, et al. Reversing chemoresistance by small molecule inhibition of the translation initiation complex eIF4F. Proc Natl Acad Sci, 2011, 108(3): 1046-1051.
[2]. Liao G, Liu G. Immediate translation of Formin DIAPH1 mRNA after its exiting the nucleus is required for its perinuclear localization in fibroblasts. PLoS One, 2013, 8(6): e68190.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt478.45
Cas No.328998-25-0
FormulaC28H18N2O6
Solubility≥23.85mg/mL in DMSO
Chemical Name(E)-4-(3-((5-(4-nitrophenyl)furan-2-yl)methylene)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrrol-1-yl)benzoic acid
SDFDownload SDF
Canonical SMILESC1=CC=C(C=C1)C2=CC(=CC3=CC=C(O3)C4=CC=C(C=C4)[N+](=O)[O-])C(=O)N2C5=CC=C(C=C5)C(=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

HL-1 cardiomyocytes

Preparation method

The solubility of this compound in DMSO is >23.85mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

5 μM;12 hr

Applications

In HL-1 cardiomyocytes, suppression of eIF4E-induced translation by 4E1RCat contributed to suppression of MCL-1 expression.

Animal experiment [2]:

Animal models

mice bearing Pten+/-Eμ-Myc or Tsc2+/-Eμ-Myc lymphomas

Dosage form

4E1RCat (15 mg/kg daily for 5 d); doxorubicin (once at 10 mg/kg on day two) intraperitoneal (i.p.) injection in 5.2% PEG 400/ 5.2% Tween 80

Application

In mice bearing Pten+/-Eμ-Myc or Tsc2+/-Eμ-Myc lymphomas, 4E1RCat and doxorubicin (Dox) synergized and extended tumor-free remissions for up to 14d, unlikely due to 4E1RCat nonspecifically increasing Dxr efficacy. 4E1RCat + Dxr increased the number of apoptotic cells. 4E1RCat decreased levels of Mcl-1 in tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Arnold N1, Koppula PR1, Gul R2, et al. Regulation of cardiac expression of the diabetic marker microRNA miR-29. PLoS One. 2014 Jul 25;9(7):e103284.

[2]. Cencic R, Hall DR, Robert F, et al. Reversing chemoresistance by small molecule inhibition of the translation initiation complex eIF4F. Proc Natl Acad Sci, 2011, 108(3): 1046-1051.

Biological Activity

Description 4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction.
Targets            
IC50            

Quality Control

Chemical structure

4E1RCat