EZH2 inhibitor III

EZH2 inhibitor III is a non-specific designation that primarily refers to two distinct research-grade inhibitors of the Polycomb Repressive Complex 2 (PRC2) sold under this catalog name by MilliporeSigma (Calbiochem). Most commonly, it refers to GSK126 (GSK2816126), a highly potent, selective, and S-adenosyl methionine (SAM)-competitive small molecule inhibitor of EZH2 methyltransferase activity. Alternatively, it can refer to SAH-EZH2, a stabilized alpha-helical 27-mer peptidomimetic that disrupts the protein-protein interaction between EED (embryonic ectoderm development) and EZH2/EZH1. While GSK126 was previously evaluated in Phase 1 clinical trials for refractory non-Hodgkin lymphoma, multiple myeloma, and solid tumors, development was terminated due to insufficient clinical efficacy. Both compounds remain widely utilized as preclinical research tools to investigate epigenetic regulation, histone H3K27 methylation, and tumor progression.

Other names

Ezh2 Inhibitor III, GSK126Ezh2 Inhibitor III, SAH-EZH2