An inhibitor of SETD8 (IC50 = 0.5 µM) that suppresses monomethylation of H4K20 in vitro; less potently inhibits Cdk4 (IC50 = 6 µM for Cdk4/cyclin D1); suppresses the expression of Cdc7

Ryuvidine – 10 mg

Brand:
Cayman
CAS:
265312-55-8
Storage:
-20
UN-No:
Non-Hazardous - /

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.{26934} It less potently inhibits cyclin-dependent kinase 4 (Cdk4; IC50 = 6 µM for Cdk4/cyclin D1).{30784} 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.{26934,30783}  

 

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Description

An inhibitor of SETD8 (IC50 = 0.5 µM) that suppresses monomethylation of H4K20 in vitro; less potently inhibits Cdk4 (IC50 = 6 µM for Cdk4/cyclin D1); suppresses the expression of 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

Synonyms:  Cdk4 Inhibitor III|Cyclic-dependent Kinase 4 Inhibitor III|SPS812

Molecular weight: 284.3

CAS: 265312-55-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Cell Biology|Cell Cycle||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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