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Ryuvidine is an inhibitor of SETD8 (IC50 = 0.5 µM) that suppresses monomethylation of H4K20 in vitro.1 It less potently inhibits cyclin-dependent kinase 4 (Cdk4; IC50 = 6 µM for Cdk4/cyclin D1).2 Over several hours of treatment, ryuvidine suppresses the expression of cell division cycle 7-related kinase (Cdc7), resulting in an ATM-dependent checkpoint response and arrest of cell cycling in S phase.1,3
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