MSC2530818 (MSC 2530818, MSC-2530818) is a potent, selective, and orally bioavailable CDK8 inhibitor with IC50 of 2.6 nM.
MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM), and displays good selectivity profile in a 264 kinase panel with exception of GSK3α (IC50=691 nM).
MSC2530818 potently inhibits of phospho-STAT1 S727 in SW620 cells (IC50=8 nM), shows potent inhibition of WNT-dependent transcription in human cancer cell lines.
MSC2530818 demonstrates tumor growth inhibition in an APC mutant SW620 human colorectal carcinoma xenograft model.
