CDK1/2/4-IN-1

CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 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].

Signaling Pathways >> Apoptosis >> Bcl-2 Family

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> Caspase

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

CDK1:1.47 (IC50)

CDK2:0.78 (IC50)

CDK4:0.87 (IC50)

Caspase 3

Bax

Bcl-2

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 IC50 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.

[1]. Farghaly TA, et, al. Discovery of thiazole-based-chalcones and 4-hetarylthiazoles as potent anticancer agents: Synthesis, docking study and anticancer activity. Bioorg Chem. 2020 May;98:103761.