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, at concentrations ranging from 0.1 to 10 μM over 72 hours, effectively inhibits the proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines with IC50 values of 0.96 μM and 0.52 μM, respectively [1]. Additionally, GL0388 demonstrates potent anti-proliferative effects across 60 human tumor cell lines at concentrations between 0.01 to 100 μM, showing GI50 values ranging from 0.299 to 1.57 μM [1]. At 1 to 10 μM over 48 hours, it significantly enhances the levels of cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells, indicating apoptosis induction [1]. Moreover, at concentrations of 0.1 to 1 μM for 24 hours, it curbs colony formation and invasion of breast cancer cells [1]. Furthermore, GL0388 promotes the insertion of Bax into the mitochondrial membranes of MDA-MB-231 cells in a concentration-dependent manner within 24 hours at 1 to 10 μM and elevates cytochrome c levels in the cytosol, suggesting the activation of apoptotic pathways [1].

GL0388, administered at doses ranging from 10-20 mg/kg intraperitoneally (i.p.) and 15 mg/kg intratumorally (i.t.), once daily for 10 days, dose-dependently reduced the growth of MDA-MB-231 tumors in female nude mice. The study utilized mice injected with MDA-MB-231 cells, showing significant tumor growth inhibition. Intratumoral administration at 15 mg/kg led to a 55% inhibition rate, demonstrating comparable efficacy to the 20 mg/kg daily intraperitoneal dose.