计算溶液所需的质量、体积或浓度。
TCH-165 is a small molecule modulator of proteasome assembly , which increases 20S levels and facilitates 20S -mediated protein degradation
In Vitro
TCH-165 (0.01-10 μM; 72 hours; RPMI8226 and U87MG cells) treatment inhibits cell growth of RPMI8226 and U87MG cells with IC 50 of 1.6 μM and 2.4 μM, respectively. ?\nTCH-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. ?\nTCH-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. ?\nTCH-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. ?\nTCH-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell Line: HEK293T cells Concentration: 0 μM, 3 μM, 10 μM Incubation Time: 24 hours Result: Enhanced proteolytic degradation in a concentration-dependent manner.
Form:Solid
IC50& Target:Proteasome assembly
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 苯丙素类和聚酮类 |
| 类(Class) | 芪类 |
| 亚类(Subclass) | 暂无 |
| 中间层级节点(Intermediate Tree Nodes) | 暂无 |
| 直接上位类(Direct Parent) | 芪类 |
| 其他上位类(Alternative Parents) | 苯苄明 α氨基酸及其衍生物 茴香醚 苯烷基胺 苯氧基化合物 苄胺 甲氧基苯 苯胺和取代苯胺 仲烷基芳胺 烷基芳基醚 咪唑内酰胺类 咪唑啉 羧酸酯 甲脒类 甲脒类 炔丙基型1,3-偶极有机化合物 一元羧酸及其衍生物 氮杂环化合物 羰基化合物 碳氢化合物衍生物 有机氧化物 |
| 分子骨架(Molecular Framework) | 芳香族杂单环化合物 |
| 取代基(Substituents) | 2-碘苯酚 - 芳基醚 - α-氨基酸或其衍生物 - 氨基脒 - 氨基酸 - 氨基酸或其衍生物 - 苯胺或取代苯胺 - 茴香醚 - 芳烷基胺 - 芳香族杂单环化合物 - 氮杂环 - 苯基化合物 - 苄胺 - 羰基 - 羧酰亚胺 - 羧酰胺基 - 羧酸衍生物 - 羧酸酰胺 - 乙醚 - 烃衍生物 - 咪唑内酰胺 - 甲氧基苯 - 单羧酸或其衍生物 - 单环苯基基团 - 有机1,3-双极性化合物 - 有机硝基化合物 - 有机氧化物 - 有机氧化合物 - 有机杂环化合物 - 有机氮化合物 - 有机氧化合物 - 苯酚醚 - 苯氧基化合物 - 苯基乙醛 - 苯基苯胺 - 苯甲胺 - 丙炔型1,3-双极性有机化合物 - 二级脂肪族/芳香族胺 - 醛基 - 苯乙烯 |
| 描述(Description) | 该化合物属于苯乙烯类有机化合物。这类化合物含有1,2-二苯基乙烯基片段。苯乙烯类(C6-C2-C6)由常见的苯丙烯(C6-C3)骨架结构衍化而来。向苯环引入一个或多个羟基可形成苯乙烯类化合物。 |
| 外部描述符(External Descriptors) | 暂无 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|