CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC 50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1 SER727 with an IC 50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC 50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.
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