Inhibitor of SETD8 protein lysine methyltransferase (PKMT) (IC50
= 0.5 μ
M); suppresses H4K20 monomethylation in vitro
. Also inhibits cyclin-dependent kinase (CDK) 4 (IC50
= 6.0 μ
M at CDK4/cyclin D1). Induces S phase accumulation in HEK293T cells. Cytotoxic against a range of human cancer cells.
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All Tocris products are intended for laboratory research use only.
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.
Ryu et al.
Small-molecule inhibitors of SETD8 with cellular activity.
Blum et al.
ASC.Chem.Biol. [Epub ahead of print], 2014;9:2471
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