naphthofluorescein

Naphthofluorescein is a synthetic small-molecule probe that acts as a cell-permeable inhibitor of the proprotein convertase furin and disrupts the interaction between hypoxia-inducible factor-1 (HIF-1) and Munc18-1-interacting protein 3 (Mint3). By blocking the Mint3–FIH-1 interaction, it suppresses Mint3-dependent HIF-1 transcriptional activity and glycolytic reprogramming in cancer cells and macrophages. In preclinical models, naphthofluorescein has demonstrated the ability to attenuate tumor growth, metastasis, and inflammatory cytokine production (such as in endotoxic shock) without significant systemic toxicity. Additionally, it functions as a pH-sensitive fluorescent dye, making it a valuable tool for intracellular pH imaging and Cerenkov-based functional imaging.

Other names

3,11-dihydroxy-spiro[7H-dibenzo[c,h]xanthene-7,1'(3'H)-isobenzofuran]-3'-onenaphthofluorescein