PT-262 是一种有效的ROCK抑制剂，IC50值约为 5 μM。PT-262 诱导线粒体膜电位的丧失并提高 caspase-3 的激活和细胞凋亡。PT-262 通过 p53 独立途径抑制ERK和CDC2磷酸化。PT-262 阻断细胞骨架功能和细胞迁移。PT-262 具有抗癌活性。
| 生物活性 | PT-262 is a potentROCKinhibitor with anIC50value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation andapoptosis. PT-262 inhibits theERKandCDC2phosphorylation via a p53-independent pathway. PT-262 blockscytoskeletonfunction and cell migration. PT-262 has anti-cancer activity[1][2]. |
| IC50& Target[1][2] | |
体外研究
(In Vitro) | PT-262 (5-40 μM; 24 小时) 在人肺癌细胞中诱导细胞毒性和增殖抑制[1]。
PT-262 (2-20 μM; 4-24小时) 在肺癌细胞中诱导 caspase-3 激活、线粒体功能障碍和细胞凋亡[1]。
PT-262 (10-20 μM; 24小时) 在 p53-wild 型和 p53-null 肺癌细胞中诱导 G2/M 期的积累，并抑制 CDC2 蛋白的磷酸化[1]。
PT-262 (0-10 μM; 24小时) 抑制肺癌细胞中的 ERK 磷酸化[1]。
PT-262 (2 μM; 24小时) 诱导肺癌 A549 细胞的细胞骨架改变和细胞伸长[2]。
PT-262 (2-10 μM; 6小时) 以浓度依赖性方式显着阻断细胞迁移[2]。
Cell Viability Assay[1] | Cell Line: | A549 cells | | Concentration: | 5-40 μM | | Incubation Time: | 24 h | | Result: | Reduced the cell viability via a concentration-dependent manner in A549 cells.
The IC50value toward human normal lung fibroblast was >20 μM. |
Apoptosis Analysis[1] | Cell Line: | A549 cells | | Concentration: | 2-20 μM | | Incubation Time: | 4-24 h | | Result: | The apoptotic cells were increased after treatment at 10 μM for 8-24 h.
The active forms of caspase-3 (12 and 17 kD) were induced following treatment with 2-20 μM for 24 h. |
Cell Cycle Analysis[1] | Cell Line: | A549 and H1299 cells | | Concentration: | 10-20 μM | | Incubation Time: | 24 h | | Result: | Significantly decreased the G1 fractions while increased the G2/M fractions in both A549 and H1299 cells with 10 μM for 24 h.
Decreased the protein levels of cyclin B1 and phospho-CDC2 at Thr14, Tyr15, and Thr161 via a concentration-dependent manner in A549 cells. |
Western Blot Analysis[1] | Cell Line: | A549 cells | | Concentration: | 0-10 μM | | Incubation Time: | 24 h | | Result: | Significantly inhibited the phosphorylation of ERK. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
