1H-Imidazole-4-carboxylic acid, 4,5-dihydro-2-(4-methoxyphenyl)-4-phenyl-1-(phenylmethyl)-5-[4-[(phenylmethyl)amino]phenyl]-, ethyl ester, (4R,5R)-rel-
1H-Imidazole-4-carboxylic acid, 4,5-dihydro-2-(4-methoxyphenyl)-4-phenyl-1-(phenylmethyl)-5-[4-[(phenylmethyl)amino]phenyl]-, ethyl ester, (4R,5R)-rel-
![1H-Imidazole-4-carboxylic acid, 4,5-dihydro-2-(4-methoxyphenyl)-4-phenyl-1-(phenylmethyl)-5-[4-[(phenylmethyl)amino]phenyl]-, ethyl ester, (4R,5R)-rel- 结构式](https://img.chemicalbook.com/CAS/20200611/GIF/1446350-60-2.gif)
1H-Imidazole-4-carboxylic acid, 4,5-dihydro-2-(4-methoxyphenyl)-4-phenyl-1-(phenylmethyl)-5-[4-[(phenylmethyl)amino]phenyl]-, ethyl ester, (4R,5R)-rel- 性质
| 沸点 | 724.6±70.0 °C(Predicted) |
|---|---|
| 密度 | 1.14±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：250 mg/mL（419.65 mM） |
| 酸度系数(pKa) | 7.15±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
1H-Imidazole-4-carboxylic acid, 4,5-dihydro-2-(4-methoxyphenyl)-4-phenyl-1-(phenylmethyl)-5-[4-[(phenylmethyl)amino]phenyl]-, ethyl ester, (4R,5R)-rel- 用途与合成方法
Proteasome assembly
TCH-165 (0.01-10 μM; 72 hours; RPMI8226 and U87MG cells) treatment inhibits cell growth of RPMI8226 and U87MG cells with IC50 of 1.6 μM and 2.4 μM, respectively.
TCH-165 (0-10 μM; 24 hours; HEK293T cells) treatment enhances ODC degradation is blocked by BTZ indicated that this event is proteasome-mediated. TCH-165 enhances proteolytic degradation in a concentration-dependent manner.
TCH-165 enhances the chymotrypsin-like (CT-L), trypsin-like (Tryp-L) and caspase-like (Casp-L) activities with EC
50
s of 4.2 μM, 3.2 μM and 4.7 μM, respectively.
TCH-165 enhances 20S-mediated degradation of IDPs, α-syn, and tau in vitro, and does not induce the degradation of structured proteins such as GAPDH.
TCH-165-treated cells display a decrease in the assembled 26S and an increase in the 20S proteasome. TCH-165 regulates the dynamic equilibrium between the 20S and 26S proteasome complexes, favoring 20S-mediated protein degradation.
Cell Viability Assay
| Cell Line: | RPMI8226 and U87MG cells |
| Concentration: | 0.01-10 μM |
| Incubation Time: | 72 hours |
| Result: | Inhibited cell growth of RPMI8226 and U87MG cells with IC 50 of 1.6 μM and 2.4 μM, respectively. |
Western Blot Analysis
| Cell Line: | HEK293T cells |
| Concentration: | 0 μM, 3 μM, 10 μM |
| Incubation Time: | 24 hours |
| Result: | Enhanced proteolytic degradation in a concentration-dependent manner. |
