WK500B is a potent and orally active BCL6 inhibitor with a KD of 1.61 µM. WK500B engages intracellular BCL6 and disrupts BCL6-corepressor interactions to reactivate BCL6 target genes. WK500B exerts cytotoxicity against diffuse large B-cell lymphoma cells and induces apoptosis and cell cycle arrest. WK500B suppresses germinal center formation in C57BL/6 mice and DLBCL tumor growth in SCID xenograft models without observable toxicity. WK500B can be used for the study of diffuse large B-cell lymphoma (DLBCL)[1].