EPZ005687 inhibits the growth of EZH2-activating-mutant lymphoma cells, with lesser effect on wild-type lymphoma, making it the first-in-class chemical probe for evaluating the effect of inhibiting EZH2 enzymatic activity in cancer. EPZ005687 is also effective in inhibiting the proliferation and migration of synovial sarcoma cells driven by a translocation in SWI/SNF subunit SS18 (242). Here, SMARCA1 is linked to cancer.