1446350-60-2

中文名称 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-

英文名称 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 1446350-60-2

分子式 C39H37N3O3

分子量 595.73

MOL 文件 1446350-60-2.mol

更新日期 2023/03/13 18:03:55

1446350-60-2 结构式

基本信息物理化学性质图谱信息常见问题列表

基本信息

中文别名

化合物TCH-165

英文别名

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-

物理化学性质

沸点724.6±70.0 °C(Predicted)

密度1.14±0.1 g/cm3(Predicted)

储存条件-20°C储存

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

图谱信息

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-(1446350-60-2)核磁图(¹HNMR)

常见问题列表

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。

靶点

Proteasome assembly

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.