Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

PROTAC CARM1 degrader-2 (compound 3e), with a DC50 value of 8.8 nM, is a VHL- and proteasome-dependent degrader of co-activator associated argininemethyltransferase (CARM1). It not only promotes the degradation of CARM1 but also prevents the methylation of its substrates, including poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, which consequently inhibits breast cancer cell migration [1].

IHMT-EZH2-426 (compound 38) is a potent, covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for EZH2 wild-type, 1.2 nM for EZH2-A687V, and 1.7-3.5 nM for EZH2-Y641F/Y641N/Y641S mutants. The compound effectively inhibits proliferation in B-cell lymphoma and triple-negative breast cancer (TNBC) cell lines, attributed to its capacity to diminish H3K27me3 and EZH2 levels [1].

EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.

CARM1-IN-1 (CARM1-IN-7G) is a selective inhibitor of CARM1 with IC50 of 8.6 μM. CARM1-IN-1 shows weak activity against PRMT1 and SET7 with IC50 > 600 μM.