GlyH-101

GlyH-101 is a cell-permeable glycine hydrazide small molecule that acts as a potent and selective inhibitor of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. Discovered through high-throughput screening, it binds to the external pore of the CFTR channel, effectively blocking chloride transport with a Ki of approximately 4.5 μM. While primarily utilized as a pharmacological tool in research to study CFTR physiology and pathology, studies have also explored its potential anti-tumor effects, demonstrating its ability to suppress proliferation, block invasion, and induce apoptosis in certain cancer cell lines, such as HT-29 colorectal cancer cells. It has also been investigated in preclinical models for the treatment of secretory diarrheas and polycystic kidney disease.

Other names

N-(2-naphthalenyl)-[(3,5-dibromo-2,4-dihydroxyphenyl)methylene]hydrazinecarboxamideGlycine hydrazide 101