GL0388 is a Bax activator and leads to Bax insertion into mitochondrial membrane that induce Bax-mediated apoptosis. GL0388 inhibits tumor growth of breast cancer xenograft in vivo which also exhibits antiproliferative activities against a variety of cancer cells with IC50 values of 0.299-1.57 μM [1].

GL0388 (0.1-10 μM; 72 h) inhibits the cell proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines, with IC 50 s of 0.96 μM and 0.52 μM, respectively [1]. GL0388 (0.01-100 μM) inhibits the cell proliferation in 60 human tumor cell lines, with GI5 50 s of 0.299-1.57 μM [1]. GL0388 (1-10 μM; 48 h) significantly upregulates the cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells [1]. GL0388 (0.1-1 μM; 24 h) inhibits the colony formation and invasion of breast cancer cells [1]. GL0388 (1-10 μM; 24 h) promotes Bax insertion into mitochondrial membranes of MDA-MB-231 cells in a dose-dependent manner. GL0388 increases cytochrome c in the cytosolic fraction of MDA-MB-231 cells [1]. Cell Proliferation Assay [1] Cell Line: MCF-7, MDA-MB-231 cells Concentration: 0.1, 0.33, 1, 3.3, 10 μM Incubation Time: 72 hours Result: Inhibited the growth of MCF-7, MDA-MB-231 cells, with IC 50 s of 0.52 μM and 0.96 μM, respectively. Western Blot Analysis [1] Cell Line: MDA-MB-231 cells Concentration: 1, 5, 10 μM Incubation Time: 48 hours Result: Significantly led to the upregulation of cleaved PARP-1 and cleaved caspase 3.

GL0388 (10-20 mg/kg for i.p.; 15 mg/kg for i.t.; once daily for 10 days) dose-dependently suppresses the growth of MDA-MB-231 tumors in mice [1]. Animal Model: Female nude mice were injected MDA-MB-231 cells [1] Dosage: 10-20 mg/kg for i.p.; 15 mg/kg for i.t. Administration: I.p and i.t. once daily for 10 days Result: Significantly inhibited tumor growth at a dose of 15 mg/kg every other day. I.T. administration for 10 consecutive days, with an inhibition rate of 55%, comparable to the I.P. efficacy at the dose of daily 20 mg/kg.