SET and diffuse large B-cell lymphoma: GSK2816126 that shows more than a 1000-fold higher selectivity of EZH2 than for other 20 human methyltransferases containing SET or non-SET domains, and effectively inhibits the proliferation of EZH2 mutants in diffuse large B-cell lymphoma cell lines and the growth of EZH2-mutant diffuse large B-cell lymphoma xenografts in mice [140].