[CAS NO. 315706-13-9] 4EGI-1
PRODUCTS SPECIFICATIONS [315706-13-9]
DESCRIPTION [315706-13-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 451.28 |
| Molecular Formula | C18H12Cl2N4O4S |
| SMILES | O=C(O)/C(CC1=CC=CC=C1[N+]([O-])=O)=N/NC2=NC(C3=CC=C(Cl)C(Cl)=C3)=CS2 |
8 Publications Citing Use of MCE
- [1]Sci Adv. 2022 Jun 24;8(25):eabo1782.
- [2]Nat Commun. 2017 Jun 8;8:15617.
- [3]Nucleic Acids Res. 2022 Jul 18;gkac611.
- [4]Cell Death Dis. 2020 Nov 15;11(11):982.
- [5]Mol Cancer Ther. 2018 Dec;17(12):2676-2688.
- [6]J Mol Med (Berl). 2019 Aug;97(8):1183-1193.
- [7]Research Square Print. 2022 Jun.
- [8]Patent. US20210299105A1.
Summary
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a K d of 25 μM against eIF4E binding.
IC50 & Target
Kd: 25 μM (eIF4E/eIF4G) [1]
In Vitro
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a K d of 25 μM against eIF4E binding. 4EGI-1 disrupts the eIF4F complex and inhibits expression of oncogenic proteins in mammalian cells. 4EGI-1 (0-40 μM) also exhibits proapoptotic activity and inhibits the growth of multiple cancer cell lines [1] . 4EGI-1 is cytotoxic to breast cancer cells, such as SKBR-3, MCF-7 and MDA-MB-231 cells, with the IC 50 of appr 30 μM, and to the non-CSCs (Cancer stem cells), the IC 50 is about 22 μM. 4EGI-1 enhances breast CSC differentiation (40 μM), and suppresses breast CSC induced HUVEC tube-like structure formation (8 μM). Moreover, 4EGI-1 selectively inhibits translation that persists in CSC maintenance and dissemination [2] . 4EGI-1 (50 µM) impairs the formation of eIF4F complex in U87 cells. 4EGI-1 (10, 50 and 100 µM) inhibits cell proliferation via inducing apoptosis in U87 cells, and the apoptosis is via Bax activation. 4EGI-1 causes mitochondrial dysfunction, and induces ER stress via GRP-78 activation, in U87 cells [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
4EGI-1 (75 mg/kg, i.p.) inhibits breast cancer stem cells (CSC) tumor growth and tumorangiogenesis in vivo [2] . 4EGI-1 (75 mg/kg, i.p.) shows inhibitory effect on the tumor volume and weight in mice bearing U87 cells [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 35 mg/mL ( 77.56 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2159 mL | 11.0796 mL | 22.1592 mL |
| 5 mM | 0.4432 mL | 2.2159 mL | 4.4318 mL |
| 10 mM | 0.2216 mL | 1.1080 mL | 2.2159 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.54 mM); Suspended solution; Need ultrasonic
References
- [1] Moerke NJ, et al. Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. Cell. 2007 Jan 26;128(2):257-67.
- [2] Yi T, et al. 4EGI-1 targets breast cancer stem cells by selective inhibition of translation that persists in CSC maintenance, proliferation and metastasis. Oncotarget. 2014 Aug 15;5(15):6028-37.
- [3] Wu M, et al. Anti-Cancer Effect of Cap-Translation Inhibitor 4EGI-1 in Human Glioma U87 Cells: Involvement of Mitochondrial Dysfunction and ER Stress. Cell Physiol Biochem. 2016;40(5):1013-1028. Epub 2016 Dec 12.