H172

H172 is a novel, potent, selective, and irreversible small-molecule inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Developed by researchers at the University of Hawaii at Manoa, Cedars-Sinai Medical Center, and the spinout Novella, H172 belongs to a class of azetidine-based compounds. It selectively and covalently binds to the DNA-binding domain (DBD) of STAT3 (specifically at Cys426), inhibiting its DNA-binding activity and Tyr phosphorylation with sub-micromolar potency (IC50 of approximately 0.98 µM). In preclinical models of triple-negative breast cancer (TNBC), H172 blocks constitutive and ligand-induced STAT3 activation, induces a misfolded protein response, endoplasmic reticulum (ER) stress, and mitophagy, ultimately leading to apoptosis and tumor growth inhibition.

Other names

STAT3-IN-8STAT-3-IN-8STAT 3-IN-8compound 9fcompound9fcompound-9f