Figures & data
Figure 3. The anti-proliferative activity of new synthetic compounds is mainly mediated by CDK9. (A) 2g inhibited the phosphorylation of Rb and RNA polymerase II, induced apoptosis through down-regulation of Mcl-1 and c-Myc protein. MIA PaCa-2 cells were incubated with or without 2g at indicated concentration for 6 h. (B) CDK9 was dose-dependently knockdown by its specific siRNA after 48 h treatment in MIA PaCa-2 cells. (C) Downregulation of CDK9 using siCDK9 (50 nM) decreased the sensitivity of MIA PaCa-2 cell to compound 2g (0.2 µM). The cells were incubated with 2g for 72 h. NS no significance; ***p < 0.001; ****p < 0.0001. Whole-cell lysates were subjected to immunoblotting. A representative protein band of three independent experiments is shown. (D) Representative illustration of the binding of synthetic compound to CDK9/cyclin T. Small molecules 1 (left column), 2g (middle column), and 2i (right column) were shown in stick representation with carbons colored yellow.
Table 1. Anti-proliferative activity of 2-((4-sulfamoylphenyl)amino)-pyrrolo[2,3-d]pyrimidine derivatives in pancreatic cancer MIA PaCa-2 cell culture.