HDACs/EZH2-IN-1

HDACs/EZH2-IN-1 (Compound 22a) is a dual inhibitor of HDACs and EZH2, exhibiting potent inhibitory activity, with EZH2 Y641N being suppressed by 98% at 50 nM. It selectively targets HDAC1 and HDAC6, with IC50 values of 0.23 μM and 0.07 μM, respectively. HDACs/EZH2-IN-1 effectively inhibits the proliferation of diffuse large B-cell lymphoma cells harboring EZH2 mutations and various acute myeloid leukemia cells. Additionally, this compound has the capability to induce cellular differentiation and apoptosis (Apoptosis) .