MS1943

MS1943 is a first-in-class, orally bioavailable proteolysis-targeting chimera (PROTAC) designed to selectively degrade Enhancer of Zeste Homolog 2 (EZH2). EZH2 is the primary methyltransferase of the Polycomb Repressive Complex 2 (PRC2), which catalyzes the trimethylation of histone H3 lysine 27 (H3K27me3), a key epigenetic modification associated with gene silencing. Unlike traditional EZH2 inhibitors that only block enzymatic activity, MS1943 utilizes a hydrophobic tagging approach to induce the proteasomal degradation of the entire EZH2 protein. This mechanism is particularly effective in cancers where EZH2 has non-enzymatic roles or where traditional inhibitors fail. MS1943 has demonstrated significant potency and high selectivity for EZH2 over EZH1 and has shown promising anticancer activity in preclinical models of triple-negative breast cancer (TNBC) and Burkitt's lymphoma.

Other names

CAS 2225938-17-8CAS2225938-17-8CAS-2225938-17-8