1018454-97-1
中文名称
Thienopyridone
英文名称
Thienopyridone
CAS
1018454-97-1
分子式
C13H10N2OS
分子量
242.3
MOL 文件
1018454-97-1.mol
更新日期
2023/03/20 15:41:25
1018454-97-1 结构式
物理化学性质
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Solid
颜色Yellow to brown
常见问题列表
生物活性
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。靶点
IC50: 173 nM (PRL-1), 277 nM (PRL-2) and 128 nM (PRL-3)
体外研究
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. |