Ryuvidine

SET domain-containing protein 8 (SETD8) is a methyltransferase that selectively monomethylates histone H4 at lysine residue 20 (H4K20), an event proven to have an important role in chromatin structure and transcriptional activation. It is also a regulator of p53, mono-methylating lysine 382 of the tumor suppressor. Ryuvidine is an inhibitor of SETD8 (IC50 = 0.5 µM) that suppresses monomethylation of H4K20 in vitro. It less potently inhibits cyclin-dependent kinase 4 (Cdk4, IC50 = 6 µM for Cdk4/cyclin D1). 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.Formal Name: 2-methyl-5-[(4-methylphenyl)amino]-4,7-benzothiazoledione. CAS Number: 265312-55-8. Synonyms: Cdk4 Inhibitor III, Cyclic-dependent Kinase 4 Inhibitor III, SPS812. Molecular Formula: C15H12N2O2S. Formula Weight: 284.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml, DMSO: 2 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 253, 531 nm. SMILES: CC1=CC=C(NC2=CC(C(SC(C)=N3)=C3C2=O)=O)C=C1. InChi Code: InChI=1S/C15H12N2O2S/c1-8-3-5-10(6-4-8)17-11-7-12(18)15-13(14(11)19)16-9(2)20-15/h3-7,17H,1-2H3. InChi Key: HFPLHASLIOXVGS-UHFFFAOYSA-N.