MKT-077 is primarily investigated for its potential as an anticancer agent due to its ability to selectively accumulate in the mitochondria of cancer cells. It functions as a cationic rhodamine analog that disrupts mitochondrial function, leading to reduced ATP production and induction of cell death in tumor cells. Its selective toxicity toward cancer cells with minimal effects on normal cells makes it a promising candidate for targeted cancer therapy. Research has also explored its use in combination with other anticancer drugs to enhance therapeutic efficacy and overcome drug resistance. Additionally, MKT-077 has been used as a fluorescent probe in cellular imaging studies to monitor mitochondrial membrane potential and assess mitochondrial health in live cells.