Novel TRPM7 Inhibitors Curb Breast Cancer Growth and Invasion in Preclinical Models
- Building on the TRPM7 blocker NS8593, researchers created a set of 2-aminobenzimidazole analogues and identified two standout leads, SDUY212 and SDUY225, validated by electrophysiological recordings.
- Both compounds slowed growth, migration and invasion in MCF-7 and MDA-MB-231 breast cancer cells and triggered apoptosis and cell-cycle arrest; SDUY212 also shrank tumors in xenograft-bearing mice.
- The anti-invasive effect appeared linked to reduced EGF-triggered STAT3 activation downstream of TRPM7.
💡 Points
Actually running electrophysiology on the leads, not just IC50s from a fluorescence assay, is what makes me trust this series — ion channel hits die in droves from off-target and assay artifacts. Still, I'd want a TRPM6/TRPM8 selectivity panel before calling SDUY212 a real chemical probe; TRPM7 has essentially none, and the 2-aminobenzimidazole scaffold looks synthetically forgiving enough to actually chase that SAR.