Thienopyridone
| 中文名称 | Thienopyridone |
|---|---|
| 中文同义词 | 化合物 T13146 |
| 英文名称 | Thienopyridone |
| 英文同义词 | Thienopyridone;Thieno[3,2-c]pyridin-4(5H)-one, 7-amino-2-phenyl- |
| CAS号 | 1018454-97-1 |
| 分子式 | C13H10N2OS |
| 分子量 | 242.3 |
| EINECS号 | 819-423-4 |
| 相关类别 | |
| Mol文件 | 1018454-97-1.mol |
| 结构式 |  |
Thienopyridone 性质
| 沸点 | 557.2±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.328±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 11.57±0.40(Predicted) |
| 形态 | 固体 |
| 颜色 | 黄至棕色 |
Thienopyridone 是一种有效的选择性的肝再生磷酸酶 (PRL) 磷酸酶抑制剂，对于 PRL-1，PRL-2 和 PRL-3，IC50 值分别为 173 nM，277 nM 和 128 nM。Thienopyridone 对其他磷酸酶的影响很小。Thienopyridone 可诱导 p130Cas 裂解和细胞凋亡 (apoptosis)，并具有抗癌作用。
IC50: 173 nM (PRL-1), 277 nM (PRL-2) and 128 nM (PRL-3)
Thienopyridone shows significant inhibition of tumor cell anchorage-independent growth in soft agar. The EC
50
values of the Thienopyridone are 3.29 μM and 3.05 μM for RKO and HT-29 cells, respectively.
Thienopyridone (1-75 μM; 24 hours; HeLa cells) treatment shows a dose-dependent down-regulation of total p130Cas in HeLa cells. Thienopyridone induces p130Cas and FAK cleavage leads to caspase-mediated cell apoptosis. Thienopyridone induces the cleavage of PARP and caspase-8.
Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation.
Cell Viability Assay
| Cell Line: | RKO and HT-29 cells |
| Concentration: | 0.5 μM, 1.67 μM, 5 μM, 8.33 μM |
| Incubation Time: | 14 days |
| Result: | Exhibited a dose-dependent inhibition in cancer cell anchorage-independent growth as measured by either colony number or colony size. |
Western Blot Analysis
| Cell Line: | HeLa cells |
| Concentration: | 1 μM, 5 μM, 10 μM, 25 μM, 50 μM, 75 μM |
| Incubation Time: | 24 hours |
| Result: | A dose-dependent down-regulation of total p130Cas was observed. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-128153 | Thienopyridone | 1 mg | 1363元 | |
| 2024/04/30 | HY-128153 | Thienopyridone Thienopyridone | 1018454-97-1 | 5mg | 3000元 |