YK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. It inhibits the phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. YK-2168 induces apoptosis in tumor cells, suppresses the expression of CDK9-regulated genes such as MYC and Mcl1, and inhibits tumor growth in CDX mice models. This product can be used for cancer research, including leukemia.
- Potently inhibits purified CDK9 enzymatic activity
- Exhibits high selectivity over CDK1 and CDK2
- Inhibits proliferation of MV4-11 leukemia cells
- Induces dose-dependent inhibition of tumor growth in CDX mice models
- Suppresses CDK9-regulated gene expression
- Upregulates cleaved caspase 3, indicating induced apoptosis
- Maintains a good safety profile in vivo with no significant body weight changes