CDK12-IN-2 is a potent, selective, and nanomolar CDK12 inhibitor with good physicochemical properties. It also acts as a strong CDK13 inhibitor and exhibits excellent kinase selectivity over CDK2, 9, 8, and 7. This compound inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II and can be used as a chemical probe for functional studies of CDK12.
- Potent, selective, and nanomolar CDK12 inhibitor (IC50=52 nM)
- Strong CDK13 inhibitor
- Excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7
- Inhibits phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II
- Can be used as a chemical probe for functional studies of CDK12
- Inhibits CTD Ser2 phosphorylation in SK-BR-3 cells (IC50 of 185 nM)
- Exhibits growth inhibition in SK-BR-3 cells (IC50 of 0.8 μM)