Figure 7.

Procaterol is a potent CDK12 inhibitor. A. Colony formation of gastric cancer cells with vehicle control and procaterol (0.5 μM) treatment. Representative images are shown. B. Cell viability in different types of human cancer (gastric cancer, colon cancer, esophageal cancer, and lung cancer) cell lines with vehicle control and procaterol (1 μM) treatment, the representative result of 72 h are shown. C. The binding of procaterol to CDK12 in SNU-1 cell lysates was determined using sepharose 4B and procaterol-conjugated sepharose 4B beads. D. The interaction between procaterol and CDK12 was predicted by a computational docking model. (Left) The representative images show that procaterol binds with CDK12 at kinase responsible site (ASP877) and nucleotide binding site (MET816). (Right) Ligand interaction diagram of procaterol bind with CDK12. E. The effect of procaterol on cell cycle progression of gastric cancer cells. Cells were treated with 0.5, 1 or 2 μM of procaterol and then incubated for 48 h for cell cycle analysis. F. The effect of procaterol on apoptosis in gastric cancer cells. Cells were treated with 0.5, 1 or 2 μM of procaterol and then incubated for 72 h for the Annexin-V staining assay. Representative images are shown. Data represent means ±SD. P<0.05: *, p<0.01: **, p<0.001: ***. Significance determined by two-tailed Student's t test.