901787-88-0
中文名稱
(Z)-4EGI-1
英文名稱
OTAVA-BB 7070707011
CAS
901787-88-0
分子式
C18H12Cl2N4O4S
分子量
451.28
MOL 文件
901787-88-0.mol
901787-88-0 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)668.9±65.0 °C(Predicted)
密度1.58±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 50 mg/mL (110.80 mM; ultrasonic and warming and heat to 60°C)
酸度系數(shù)(pKa)0.71±0.41(Predicted)
形態(tài)Solid
顏色Light brown to gray
常見問題列表
生物活性
(Z)-4EGI-1 是 4EGI-1 的 Z-型異構(gòu)體，是 eIF4E/eIF4G 相互作用和翻譯起始的抑制劑。(Z)-4EGI-1 有效結(jié)合 eIF4E ，IC50 為 43.5 μM，Kd 值為 8.74 μM。(Z)-4EGI-1 具有抗癌活性。靶點(diǎn)
IC50: 43.5 μM (eIF4E)
Kd: 8.74 μM (eIF4E)
體外研究
(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.
(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.
Western Blot Analysis
| 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. |