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GL0388 is a small-molecule, fluorinated activator of the pro-apoptotic protein Bax (Bcl-2-associated X protein). Developed by researchers at the University of Texas Medical Branch and Louisiana State University Health Sciences Center, GL0388 was optimized from the lead compound CYD-4-61 to improve safety and efficacy. It targets the Ser184 residue of Bax, promoting its insertion into the outer mitochondrial membrane, which triggers mitochondrial outer membrane permeabilization (MOMP), cytochrome c release, and subsequent caspase-mediated apoptosis. GL0388 has demonstrated potent antiproliferative, anti-migratory, and anti-invasive activities against various breast cancer cell lines, including triple-negative breast cancer (TNBC), and has shown significant in vivo tumor growth suppression in breast cancer xenograft models.
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