4E1RCat
(Synonyms: eIF4E/eIF4G Interaction Inhibitor II) 目录号 : GC13104
An eIF4F inhibitor
Cas No.:328998-25-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
HL-1 cardiomyocytes |
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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. |
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Reacting condition |
5 μM;12 hr |
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Applications |
In HL-1 cardiomyocytes, suppression of eIF4E-induced translation by 4E1RCat contributed to suppression of MCL-1 expression. |
| Animal experiment [2]: | |
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Animal models |
mice bearing Pten+/-Eμ-Myc or Tsc2+/-Eμ-Myc lymphomas |
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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 |
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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. |
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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. |
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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. |
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| Cas No. | 328998-25-0 | SDF | |
| 别名 | eIF4E/eIF4G Interaction Inhibitor II | ||
| 化学名 | (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 | ||
| 分子式 | C28H18N2O6 | 分子量 | 478.45 |
| 溶解度 | ≥ 23.85mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet