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Biological Activity:

Ryuvidine is a potent, selective and cell permeable lysine methyltransferase SETD8 inhibitor with IC50 ~0.5 μM. It has cellular activity by suppressing the H4K20me1 mark of SETD8 and recapitulate characteristic S/G2/M-phase cell cycle defects as observed for RNAi-mediated SETD8 knockdown. It also inhibits cyclin-dependent kinase (CDK) 4 (IC50 ~6.0 μM at CDK4/cyclin D1). SETD8's methyltransferase activity has been implicated in many essential cellular processes including DNA replication, DNA damage response, transcription modulation, and cell cycle regulation. Ryuvidine is a good tool compound to elucidate the diverse roles of SETD8.

How to Use:

In vitro: Ryuvidine was used at 10 µM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Ryu CK, et al. 5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents. (2000) Bioorg Med Chem Lett. 10(5):461-4.
• 2. Blum G, et al. Small-molecule inhibitors of SETD8 with cellular activity. (2014) ACS Chem Biol. 9(11):2471-8.