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TC-5115 is a potent inhibitor of MLL methyltransferase with IC50 value of 16 nM. TC-5115 may lead to the development of a new therapy for the treatment of human MLL leukemia. The mixed-lineage leukemia (MLL) protein, also known as MLL1, is a lysine methyltransferase specifically responsible for methylation of histone 3 lysine 4. MLL has been pursued as an attractive therapeutic target for the treatment of acute leukemia carrying the MLL fusion gene or MLL leukemia.