UNC0379
SETD8 inhibitor / UNC0379 is an inhibitor of the lysine methyltransferase SETD8 with selectivity over 15 other methyltransferases.1 IC50’s = 7.3 µM in a radioactive methyl transfer assay and 9.0 µM in an MCE assay. UNC0379 treatment of SY5Y and NGP neuroblastoma cell lines lead to activation of p53 and decreased tumor growth in an ex-vivo tumorigenicity assay.2
Biochemicals & reagents
1620401-82-2
1) Ma et al. (2014), Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8; J.Med.Chem. 57 6822 2) Veschi et al. (2017), Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma; Cancer Cell 31 50
-20°C
TARGET: Protein methyltransferase -- PATHWAY: Chromatin; Posttranslational modification; p53; Proliferation -- RESEARCH AREA: Epigenetics; Neuroscience -- DISEASE AREA: Cancer