Molecular structure of eIF4E/eIF4G Interaction Inhibitor, 4EGI-1, CAS Number: 315706-13-9
eIF4E/eIF4G Interaction Inhibitor, 4EGI-1 (CAS 315706-13-9)
See product citations (14)
Application:
eIF4E/eIF4G Interaction Inhibitor, 4EGI-1 is amplifies TRAIL-induced apoptosis via down-regulation of FLIPS/L and induction of DR5
CAS Number:
315706-13-9
Purity:
>95%
Molecular Weight:
451.3
Molecular Formula:
C18H12Cl2N4O4S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Product Citations
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
eIF4E/eIF4G Interaction Inhibitor, 4EGI-1, may act to amplify TRAIL (tumor necrosis factor-related apoptosis-inducing ligand)-induced apoptosis via down-regulation of FLIPS/L and induction of DR5. These characteristics of the compound seem to be independent of it′s ability to inhibit cap-dependent protein translation which is caused by disruption of the eIF4E/eIF4G association through binding to eIF4E. It has been shown that while eIF4E/eIF4G Interaction Inhibitor, 4EGI-1 displaces eIF4G from eIF4E, it consequentially enhances 4E-BP association both in vivo and in vitro. 4E-BPs regulated the eIF4E/eIF4G complex which has a central role in the regulation of gene expression at the level of translation initiation.
eIF4E/eIF4G Interaction Inhibitor, 4EGI-1 (CAS 315706-13-9) References
- Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G. | Moerke, NJ., et al. 2007. Cell. 128: 257-67. PMID: 17254965
- Taking aim at protein translation in AML. | Carroll, M. 2009. Blood. 114: 1458-9. PMID: 19696209
- Targeting translation in acute myeloid leukemia: a new paradigm for therapy? | Tamburini, J., et al. 2009. Cell Cycle. 8: 3893-9. PMID: 19934662
- The eIF4E/eIF4G interaction inhibitor 4EGI-1 augments TRAIL-mediated apoptosis through c-FLIP Down-regulation and DR5 induction independent of inhibition of cap-dependent protein translation. | Fan, S., et al. 2010. Neoplasia. 12: 346-56. PMID: 20360945
- Cap-translation inhibitor, 4EGI-1, restores sensitivity to ABT-737 apoptosis through cap-dependent and -independent mechanisms in chronic lymphocytic leukemia. | Willimott, S., et al. 2013. Clin Cancer Res. 19: 3212-23. PMID: 23633452
- 3-substituted indazoles as configurationally locked 4EGI-1 mimetics and inhibitors of the eIF4E/eIF4G interaction. | Yefidoff-Freedman, R., et al. 2014. Chembiochem. 15: 595-611. PMID: 24458973
- Structure-activity relationship study of 4EGI-1, small molecule eIF4E/eIF4G protein-protein interaction inhibitors. | Takrouri, K., et al. 2014. Eur J Med Chem. 77: 361-77. PMID: 24675136
- Synthesis of rigidified eIF4E/eIF4G inhibitor-1 (4EGI-1) mimetic and their in vitro characterization as inhibitors of protein-protein interaction. | Mahalingam, P., et al. 2014. J Med Chem. 57: 5094-111. PMID: 24827861
- Structure of the eukaryotic translation initiation factor eIF4E in complex with 4EGI-1 reveals an allosteric mechanism for dissociating eIF4G. | Papadopoulos, E., et al. 2014. Proc Natl Acad Sci U S A. 111: E3187-95. PMID: 25049413
- The synergistic inhibition of breast cancer proliferation by combined treatment with 4EGI-1 and MK2206. | Wang, H., et al. 2015. Cell Cycle. 14: 232-42. PMID: 25607647
- The cap-translation inhibitor 4EGI-1 induces mitochondrial dysfunction via regulation of mitochondrial dynamic proteins in human glioma U251 cells. | Yang, X., et al. 2015. Neurochem Int. 90: 98-106. PMID: 26220902
- 4EGI-1 induces apoptosis and enhances radiotherapy sensitivity in nasopharyngeal carcinoma cells via DR5 induction on 4E-BP1 dephosphorylation. | Wang, W., et al. 2016. Oncotarget. 7: 21728-41. PMID: 26942880
- Anti-Cancer Effect of Cap-Translation Inhibitor 4EGI-1 in Human Glioma U87 Cells: Involvement of Mitochondrial Dysfunction and ER Stress. | Wu, M., et al. 2016. Cell Physiol Biochem. 40: 1013-1028. PMID: 27941351
- 1H, 13C, and 15N backbone chemical shift assignments of 4E-BP144-87 and 4E-BP144-87 bound to eIF4E. | Sekiyama, N., et al. 2017. Biomol NMR Assign. 11: 187-191. PMID: 28589219
Inhibitor of:
(eukaryotic translation initiation factor) eIF, (eukaryotic translation initiation factor) eIF1, (eukaryotic translation initiation factor) eIF2, (eukaryotic translation initiation factor) eIF5, 2900097C17Rik, Cordon-bleu, CYFIP1, DDEF2, EG435337, EG666806, eIF1, eIF2Bδ, eIF3β, eIF4E, eIF4G, eIF4H, eIF5A1, FGD2, FMR1, GS2, HES1, Jaw1, Mnk1, Papilin, PRA1, SPP, and TMEM55B.Activator of:
β-catenin, ARFGAP1, DENR, EG432502, EG435337, eIF3θ, eIF4B, Paip2b, TBC1D24, TRAP-γ, UBPY, and XBP-1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
eIF4E/eIF4G Interaction Inhibitor, 4EGI-1, 10 mg | sc-202597 | 10 mg | $265.00 |