BAPT 78

BAPT 78 is a novel small molecule macropinocytosis inducer (MPI) synthesized as a derivative of the 3-(((3-mercapto-5-(pyridin-4-yl)-4H-1,2,4-triazol-4-yl)imino)methyl)quinolin-2-ol (BAPT) scaffold. It functions by stimulating macropinocytosis, a form of endocytosis that enables the non-selective uptake of extracellular fluid and macromolecules into large vesicles called macropinosomes. In preclinical research, BAPT 78 has been shown to significantly increase the intracellular delivery of high-molecular-weight dextran, albumin, and antibodies in colorectal cancer (CRC) and triple-negative breast cancer (TNBC) cell lines. Additionally, BAPT 78 acts as a chemosensitizer, enhancing the cytotoxic activity of small molecule drugs like doxorubicin and paclitaxel, including in paclitaxel-resistant cancer cells. While it effectively promotes internalization, its ability to facilitate the endosomal escape of larger macromolecules such as saporin or siRNA is limited, potentially due to low endolytic capacity.