CGP049090

CGP049090 is a **small molecule inhibitor** that selectively disrupts the interaction between β-catenin and lymphoid enhancer factor-1 (lef-1), which are key components of the Wnt/β-catenin signaling pathway[1][4]. This drug induces apoptosis in chronic lymphocytic leukemia (CLL) cells and inhibits the growth of CLL-derived tumor xenografts, with minimal impact on healthy B cells[1][3]. CGP049090 has been shown to block the β-catenin/lef-1 interaction in vitro and in vivo, leading to downregulation of lef-1 target genes such as c-myc and cyclin D1 as part of its mechanism of action[1]. CGP049090 is sometimes referred to by the alternative name "cercosporin"[7]. It is primarily in preclinical and early clinical investigation as a candidate therapy for CLL and potentially other malignancies where Wnt/β-catenin signaling is implicated.

Brand names

CGP049090CGP-049090CGP 049090

Other names

Cercosporin