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-
- CAS号:1446350-60-2
- 英文名: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-
- 中文名: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-
- CBNumber:CB35562371
- 分子式:C39H37N3O3
- 分子量:595.73
- MOL File:1446350-60-2.mol
- 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 :DMSO: 250 mg/mL (419.65 mM)
- 酸度系数(pKa) :7.15±0.70(Predicted)
- 形态 :Solid
- 颜色 :Light yellow to yellow
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、用途与生产工艺
- 生物活性 TCH-165 是蛋白酶体组装的小分子调节剂,可增加 20S 水平并促进 20S 介导的蛋白质降解。
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靶点
Proteasome assembly
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体外研究
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.
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