CDK1/2/4-IN-1 (compound 3a) 是一种有效的 CDK 抑制剂， CDK1、CDK2 和 CDK4 的IC50值分别为 1.47、0.78 和 0.87 μM。CDK1/2/4-IN-1 在 G2/M 期阻滞细胞周期并诱导细胞凋亡 (apoptosis)。CDK1/2/4-IN-1 升高 Bax、caspase-3、P53 水平，降低 Bcl-2 水平。CDK1/2/4-IN-1 可用于癌症研究。
| 生物活性 | CDK1/2/4-IN-1 (compound 3a) is a potentCDKinhibitor withIC50values of 1.47, 0.78 and 0.87 μM forCDK1,CDK2andCDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and inducesapoptosis. CDK1/2/4-IN-1 elevatesBax, caspase-3, P53 levels and decreasesBcl-2level. CDK1/2/4-IN-1 can be used forcancerresearch[1]. |
| IC50& Target[1] | CDK1 1.47 (IC50) | CDK2 0.78 (IC50) | CDK4 0.87 (IC50) | Caspase 3 | Bax | Bcl-2 |
|
体外研究
(In Vitro) | CDK1/2/4-IN-1 (compound 3a) (0.01-100 μM; 24 hours) has antitumor activity in cancer cell lines[1].
CDK1/2/4-IN-1 (compound 3a) (1.39 μM; 24 hours) induces apoptosis and arrests cell cycle at G2/M phase in A549 cells[1].
CDK1/2/4-IN-1 (compound 3a) (1.39 μM; A549 cells) induces up-regulation of the expression of Bax, caspases-3 and p53, and increases the ratio of Bcl-2[1].
Cell Cytotoxicity Assay[1] | Cell Line: | Liver cancer cell line (HepG-2), lung cancer cell line (A549) and breast cancer cell line (MCF-7) | | Concentration: | 0.01, 0.1, 1.0, 10, 100 μM | | Incubation Time: | 24 hours | | Result: | Displayed cytotoxic activity with IC50values of 1.56, 1.39 and 1.97 μM for HepG-2, A549 and MCF-7, respectively. |
Cell Cycle Analysis[1] | Cell Line: | A549 cells | | Concentration: | 1.39 μM | | Incubation Time: | 24 hours | | Result: | Increased G2/M phase by 2.6 folds compared with the control cells. |
Apoptosis Analysis[1] | Cell Line: | A549 cells | | Concentration: | 1.39 μM | | Incubation Time: | 24 hours | | Result: | Increased the overall percentage of the apoptotic cells. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 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. |
m.cnreagent.com