cdk8-in-13

CDK8-IN-13 is a CDK8 inhibitor (IC50: 51.9 nM) with potent, selective and oral activity. CDK8-IN-13 induces apoptosis and reduces the expression of p-STAT1 S727 and p-STAT5 S726. CDK8-IN-13 exhibits anti-tumour activity.

CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showed anti-proliferative activity against MV4-11 cells.

CDK8-IN-6 (compound 9) is a potent inhibitor of cyclin-dependent kinase 8 (CDK8) with a Kd of 13 nM, demonstrating significant research potential in AML cancers.

CDK8-IN-7 (compound 12) is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8), with a Kd of 3.5 nM, and has demonstrated potential for AML-cancer research.

CDK8-IN-14 (compound 12) effectively inhibits CDK8, demonstrating an IC50 of 39.2 nM, and exhibits potent anti-AML cell proliferation effects, with a GC50 value of 0.02±0.01μM in MOLM-13 cells and 0.03±0.01μM in MV4-11 cells [1].