BCL6 inhibitor 79-6 (Compound 79-6, CID5721353) is the first-generation, specific BCL6 BTB domain inhibitor with IC50 of 200 uM, Kd of 129 uM.
BCL6 inhibitor 79-6 binds to a pocket in the lateral groove of the BCL6 BTB domain, specifically inhibits BCL6 but not other BTB-ZF proteins.
BCL6 inhibitor 79-6 disrupts BCL6/corepressor complexes and reactivates BCL6 target genes in vitro and in vivo, selectively kills BCL6-dependent DLBCL cells.
BCL6 inhibitor 79-6 suppresses human DLBCL xenografts in mice with favorable pharmacokinetics.
