UNC0379 is an inhibitor of the lysine methyltransferase SETD8 with selectivity over 15 other methyltransferases.1 IC50s = 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
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