901787-88-0

901787-88-0 structure
901787-88-0 structure
  • Name: (Z)-4EGI-1
  • Chemical Name: (Z)-4EGI-1
  • CAS Number: 901787-88-0
  • Molecular Formula: C18H12Cl2N4O4S
  • Molecular Weight: 451.28
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Eukaryotic Initiation Factor (eIF)
  • Create Date: 2020-08-08 16:58:19
  • Modify Date: 2024-01-11 18:37:52
  • (Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity[1][2].

Name (Z)-4EGI-1
Description (Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity[1][2].
Related Catalog
Target

IC50: 43.5 μM (eIF4E)[2] Kd: 8.74 μM (eIF4E)[1]

In Vitro (Z)-4EGI-1 (15-30 µM; 6 hours; CRL-2813 melanoma cells) treatment markedly reduces the expressions of the regulatory proteins: cyclin D1, cyclin E, and Survivin, while the expressions of housekeeping proteins such as β-Actin and α-Tubulin are not affected[1]. (Z)-4EGI-1 inhibits cancer cells proliferation with IC50 values of 15.3 μM and 11.6 μM for CRL-2351 breast cells and CRL-2813 melanoma cells, respectively[2]. Western Blot Analysis[1] Cell Line: CRL-2813 melanoma cells Concentration: 15 µM, 30 µM Incubation Time: 6 hours Result: Markedly reduced the expressions of the regulatory proteins: cyclin D1, cyclin E, and Survivin.
References

[1]. Khuloud Takrouri, et al. Structure-activity Relationship Study of 4EGI-1, Small Molecule eIF4E/eIF4G Protein-Protein Interaction Inhibitors. Eur J Med Chem. 2014 Apr 22;77:361-77.

[2]. Poornachandran Mahalingam, et al. Synthesis of Rigidified eIF4E/eIF4G inhibitor-1 (4EGI-1) Mimetic and Their in Vitro Characterization as Inhibitors of Protein-Protein Interaction. J Med Chem. 2014 Jun 26;57(12):5094-111.

Molecular Formula C18H12Cl2N4O4S
Molecular Weight 451.28
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