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。
产品描述
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC 50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research [1].
体外活性
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 IC 50 values 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.
Cas No.
2414633-49-9
分子式
C15H16N2O2S
分子量
288.36
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years