cid5721353

Description: CID5721353 (also known as BCL6 Inhibitor and 79-6) is a novel and potent inhibitor of BCL6 (B-Cell Lymphoma 6) with an IC50 value of 212 uM (equivalent to a Ki of 147 uM). The BCL6 transcriptional repressor is the most frequently involved oncogene in diffuse large B cell lymphoma (DLBCL). It was identified by combining computer-aided drug design with functional assays to identify low-molecular-weight compounds that bind to the corepressor binding groove of the BCL6 BTB domain. One such compound disrupted BCL6/corepressor complexes in vitro and in vivo, and was observed by X-ray crystallography and NMR to bind the critical site within the BTB groove. CID5721353 could induce expression of BCL6 target genes and kill BCL6-positive DLBCL cell lines. In xenotransplantation experiments, CID5721353 was nontoxic and potently suppressed DLBCL tumors in vivo. CID5721353 also killed primary DLBCLs from human patients.

References: Cancer Cell. 2010 Apr 13; 17(4):400-11.