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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(jié)構(gòu)式 1446350-60-2 結(jié)構(gòu)式

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(xué)性質(zhì)

沸點(diǎn)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

常見問題列表

生物活性
TCH-165 是蛋白酶體組裝的小分子調(diào)節(jié)劑,可增加 20S 水平并促進(jìn) 20S 介導(dǎo)的蛋白質(zhì)降解。
靶點(diǎn)

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

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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