328998-25-0|4E1RCat|CsnPharm

CAS No.: 328998-25-0

4E1RCat Catalog No. CSN18215

Synonyms: eIF4E/eIF4G Interaction Inhibitor II

4E1RCat blocks interaction between eIF4E:eIF4G and eIF4E:4E-BP1, prevents assembly of the eIF4F complex and inhibits cap-dependent translation with IC50 ~4 μM.

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技术信息

生物活性

描述Eukaryotic translation initiation is tightly regulated at the step of ribosome recruitment. This process involves binding of eukaryotic initiation factor (eIF) 4F complex to mRNA cap structures. eIF4F is composed of: eIF4E, the cap-binding protein; eIF4A, a DEAD-box RNA helicase; and eIF4G, a scaffolding protein that bridges the interaction between eIF4E and eIF4A. 4E1RCat is an inhibitor of eIF4E:eIF4G interaction with an IC₅₀ an of ∼4 μM. It also blocks eIF4E:4E-BP1 interaction. 4E1RCat at 50 μM reduced 80S ribosome complex formation and this inhibition of ribosome recruitment to mRNA by 4E1RCat was cap-specific. 4E1RCat inhibited cap-dependent translation from FF/HCV/Ren in a dose dependent manner. It also inhibited cap-dependent production of Ren Luc from Ren/CrPV/FF. Furthermore, in Jurkat cells, 4E1RCat at 50 μM decreased polysomes, increased the fraction of 80S ribosomal subunits, and decreased levels of Mcl-1 and c-Myc proteins, two eIF4E-dependent mRNAs. In vivo, 4E1RCat (15 mg/kg daily for 5 d) could reverse chemoresistance in a Myc-driven lymphoma model, consistent with the idea that deregulated translation plays a role in this phenomenon^[3].
作用机制eIF4E has five shallow pockets that form an elongated binding site and could support small molecule interactions. 4E1RCat shows potential for binding to four of these pockets^[3].
参考文献

[1] Salomon JJ, Spahn S,et al. Generation and functional characterization of epithelial cells with stable expression of SLC26A9 Cl- channels. Am J Physiol Lung Cell Mol Physiol. 2016 Apr 1;310(7):L593-602.
[2] Muanprasat C, Sonawane ND, et al. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy. J Gen Physiol. 2004 Aug;124(2):125-37.
[3] Cencic R, Hall DR, Robert F, et al. Reversing chemoresistance by small molecule inhibition of the translation initiation complex eIF4F. Proc Natl Acad Sci U S A. 2011;108(3):1046-1051

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0901 mL
- 10.4504 mL
- 20.9008 mL
- 5 mM
- 0.4180 mL
- 2.0901 mL
- 4.1802 mL
- 10 mM
- 0.2090 mL
- 1.0450 mL
- 2.0901 mL

技术信息

CAS号

328998-25-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H18N2O6

运输

蓝冰

分子量

478.45

别名

eIF4E/eIF4G Interaction Inhibitor II

溶解度

DMSO	37.0 mg/mL (77.3 mM) warming
Water	insoluble

动物实验配方

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