4E1RCat (Synonyms: eIF4E/eIF4G Interaction Inhibitor II) |
| رقم الكتالوجGC13104 |
4E1RCat هو مثبط للترجمة المعتمدة على الغطاء ، ويثبط تفاعل eIF4E: eIF4GI ، مع IC50 و ~4 ميكرومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 328998-25-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
| 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. |
|
| Cas No. | 328998-25-0 | SDF | |
| المرادفات | eIF4E/eIF4G Interaction Inhibitor II | ||
| 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 | ||
| Canonical SMILES | C1=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 | ||
| Formula | C28H18N2O6 | M.Wt | 478.45 |
| الذوبان | ≥ 23.85mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0901 mL | 10.4504 mL | 20.9008 mL |
| 5 mM | 0.418 mL | 2.0901 mL | 4.1802 mL |
| 10 mM | 0.209 mL | 1.045 mL | 2.0901 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *