1446350-60-2

中文名稱 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-

英文名稱 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 2024/11/01 22:00:08

1446350-60-2 結構式

基本信息物理化學性質安全數(shù)據(jù) 圖譜信息 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-價格(試劑級) 常見問題列表

基本信息

中文別名

化合物TCH-165

英文別名

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-

物理化學性質

沸點724.6±70.0 °C(Predicted)

密度1.14±0.1 g/cm3(Predicted)

儲存條件-20°C儲存

溶解度DMSO: 250 mg/mL (419.65 mM)

酸度系數(shù)(pKa)7.15±0.70(Predicted)

形態(tài)Solid

顏色Light yellow to yellow

InChIKeyXXDLWRCUPASJGY-AEGYFVCZSA-N

SMILESN2([C@@H]([C@](N=C2c6ccc(cc6)OC)(c5ccccc5)C(=O)OCC)c3ccc(cc3)NCc4ccccc4)Cc1ccccc1

安全數(shù)據(jù)

WGK GermanyWGK 3

存儲類別11 - Combustible Solids

圖譜信息

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)核磁圖(¹HNMR)

常見問題列表

生物活性

TCH-165 是蛋白酶體組裝的小分子調節(jié)劑，可增加 20S 水平并促進 20S 介導的蛋白質降解。

靶點

Proteasome assembly

體外研究

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