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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-, 1446350-60-2, 结构式
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-
英文别名:
rel-Ethyl (4R,5R)-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate;Proteasome,tau,trypsin-like,20S,TCH165,IDPs,chymotrypsin-like,degradation,TCH 165,α-syn,inhibit,caspase-like,TCH-165,assembly,Inhibitor;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-
中文别名:
化合物TCH-165;REL-(4R,5R)-1-苄基-5-(4-(苄基氨基)苯基)-2-(4-甲氧基苯基)-4-苯基-4,5-二氢-1H-咪唑-4-羧酸乙酯
CBNumber:
CB35562371
分子式:
C39H37N3O3
分子量:
595.73
MOL File:
1446350-60-2.mol

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-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:
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
安全信息

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-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。

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.

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- 上下游产品信息

上游原料

下游产品


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- 生产厂家

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1446350-60-2, 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- 相关搜索:

  • 抑制剂
  • C39H37N3O3
  • REL-(4R,5R)-1-苄基-5-(4-(苄基氨基)苯基)-2-(4-甲氧基苯基)-4-苯基-4,5-二氢-1H-咪唑-4-羧酸乙酯
  • 化合物TCH-165
  • 1446350-60-2
  • Proteasome,tau,trypsin-like,20S,TCH165,IDPs,chymotrypsin-like,degradation,TCH 165,α-syn,inhibit,caspase-like,TCH-165,assembly,Inhibitor
  • rel-Ethyl (4R,5R)-1-benzyl-5-(4-(benzylamino)phenyl)-2-(4-methoxyphenyl)-4-phenyl-4,5-dihydro-1H-imidazole-4-carboxylate
  • 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-
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