MG-KKR-5-268

MG-KKR-5-268 is a novel tetrahydroisoquinoline (THIQ) analog developed by researchers at Florida A&M University as a cytostatic agent for the treatment of triple-negative breast cancer (TNBC). It is a more potent derivative of the earlier compound MG-KKR-4-53. Unlike traditional taxanes or vinca alkaloids that target microtubules, MG-KKR-5-268 exerts its effects through a non-tubulin mechanism, specifically inducing cell cycle arrest at the G2/M phase and preventing 3D tumor solidification via transcriptome reprogramming. In preclinical studies, it demonstrated significant cytostatic activity with an IC50 of 169 nM in TNBC cell lines and showed the ability to prevent tumor spheroid compaction, phenocopying the effects of vinblastine without binding to microtubules.

Other names

3-fluoro-N-(7-hydroxy-3,4-dihydroisoquinolin-2(1H)-yl)-4-methylbenzamide