Valemetostat is an orally available potent and selective inhibitor of EZH1 and EZH2 (the histone lysine methyltransferases enhancer of zeste homolog 1 and 2) (both wild-type and mutated forms) with IC50s in nanomolar concentrations. Demonstrates anti-proliferative effect against various NHL (non-Hodgkin lymphomas) cells, such as diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma, and peripheral T-cell lymphoma, with GI50 values less than 100 nM regardless of EZH2 gain-of-function mutations; Induces differentiation of undifferentiated NHL cells with increment of cell lineage specific markers and which induced cell death in vitro; Shows synergistic effect with the standard of care agents for NHL in vitro and in vivo.

KEYWORDS: Valemetostat | Supplier | EZH1/2 HMTase inhibitor | DS-3201B | CAS [1809336-39-7] | Histone | HMTase | Inhibitor | Enzymes