cdk8/cycc

SEL120-34A HCl is a selective, orally available and ATP-competitive inhibitor of CDK8(CDK8 CycC and CDK19 CycC with IC50s of 4.4 nM and 10.4 nM , respectively), with antitumor activity.

SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8 CycC, CDK19 CycC and CDK9 cycT. SEL120-34A possesses antitumor activity.

CDK8 19-IN-2 (compound 12) is a potent inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), exhibiting IC 50 values of 2.08 nM and 2.49 nM, respectively. This orally active compound is applicable in the research of acute myeloid leukemia (AML), breast cancer, and lymphoma.

CDK8 19-IN-1 is a selective, orally bioavailable dual inhibitor of CDK8 and CDK19, with IC50 values of 0.46 nM for CDK8, 0.99 nM for CDK19, and 270 nM for [CDK9].

BRD6989 is an analog of the natural product cortistatin A (dCA). Which inhibits CDK8 and upregulates IL-10. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM.