CG0009 is a potent and selective a Glycogen Synthase Kinase 3 (GSK3) inhibitor. CG0009, inhibits proliferation, induces apoptosis cell death, and activates the p53-Bax pathway in breast cancer cells, predominantly via cyclin D1 depletion. CG0009 induces significant growth inhibition and cell death in breast cancer cell lines, with a wide range of IC50 values (between 0.49 (MCF7) and 11 μM (NCI/ADR-RES and BT549)). CG0009 inhibits breast cancer cell growth through cyclin D1 depletion and p53 activation, and may thus offer an innovative therapeutic approach for breast cancers resistant to hormone-based therapy.