YK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. It inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. This compound induces apoptosis in tumor cells, suppresses the expression of CDK9-regulated genes, and inhibits tumor growth in CDX mice models. It is suitable for cancer research, including leukemia.
- Potent and selective CDK9 inhibitor (IC50 = 5.9 nM)
- Inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain
- Induces apoptosis in tumor cells
- Suppresses expression of CDK9-regulated genes (e.g., MYC and Mcl1)
- Inhibits tumor growth in CDX mice models
- High selectivity over CDK1 and CDK2
- Does not inhibit hERG channel activity at concentrations up to 30 μM
- Demonstrates a good safety profile in animal models