[CAS NO. 901787-88-0] (Z)-4EGI-1
PRODUCTS SPECIFICATIONS [901787-88-0]
DESCRIPTION [901787-88-0]
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 |
Summary
IC50 & Target
|
eIF4 |
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 IC
50
values of 15.3 μM and 11.6 μM for CRL-2351 breast cells and CRL-2813 melanoma cells, respectively
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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 : 50 mg/mL ( 110.80 mM ; ultrasonic and warming and heat to 60°C)
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.
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.