BAPT 54

BAPT 54 is a novel small molecule macropinocytosis inducer (MPI) identified as a lead compound within a series of 3-(((3-mercapto-5-(pyridin-4-yl)-4H-1,2,4-triazol-4-yl)imino)methyl)quinolin-2-ol (BAPT) derivatives. It functions by stimulating macropinocytosis, a non-selective endocytic pathway, to enhance the intracellular delivery of various therapeutic agents. Preclinical evaluations in colorectal cancer (CRC) cell lines, including SW620 and HCT116, demonstrated that BAPT 54 significantly increases the uptake of high-molecular-weight molecules such as dextran and albumin, as well as anti-tubulin antibodies. While it effectively promotes internalization, its ability to facilitate the subsequent endosomal escape of payloads like siRNA or saporin appears limited. BAPT 54 is being researched as a potential tool to overcome the plasma membrane barrier for macromolecular and small molecule drug delivery in oncology.