A-395 is an inhibitor of the interaction between embryonic ectoderm development (EED) and histone H3 lysine 27 (H3K27) that binds to the EED subunit of polycomb repressor complex 2 (PRC2) and inhibits H3K27 methylation (Ki = 0.4 nM).1 It inhibits H3K27 di- and trimethylation in RD rhabdoid tumor cells (IC50s = 390 and 90 nM, respectively). In vivo, A-395 (200 mg/kg) reduces tumor volume and intratumor H3K27 trimethylation in a Pfeiffer diffuse large B cell lymphoma (DLBCL) mouse xenograft model. See the Structural Genomics Consortium (SGC) website for more information.WARNING This product is not for human or veterinary use.
