SEL120-34A is a dual inhibitor of cyclin-dependent kinase 8 (Cdk8) and Cdk19 (IC50s = 4.4 and 10.4 nM, respectively).1 It is selective for Cdk8 and Cdk19 over a panel of CDK/cyclin complexes at 1 ?M. SEL120-34A (0.1-5 ?M) inhibits IFN-γ-induced phosphorylation of STAT1 in HCT116 colon cancer cells and the proliferation of various acute myeloid leukemia (AML) cells, including MOLM-16, MV4-11, and KG-1 cells (GI50s = <1 ?M). It reduces tumor growth in a KG-1 mouse xenograft model when administered at a dose of 60 mg/kg.
1.Rzymski, T., Mikula, M., ?y?kiewicz, E., et al.SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domainsOncotarget8(20)33779-33795(2017)