H105

H105 is an azetidine-based small molecule inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Developed by researchers at the University of Hawaii and Cedars-Sinai Medical Center, and licensed to the spinout company Novella, H105 directly and selectively inhibits STAT3 DNA-binding activity and phosphorylation at Tyr705, with an IC50 of approximately 1.75–2.07 µM in vitro. It exhibits high selectivity for STAT3 over STAT1 and STAT5. In preclinical studies, H105 has demonstrated the ability to decrease STAT3 activation, inhibit cell growth and viability, and induce apoptosis in triple-negative breast cancer (TNBC) cell lines (such as MDA-MB-231 and MDA-MB-468) harboring constitutively active STAT3. Oral administration of H105 has also been shown to suppress the growth of human breast cancer tumor xenografts in vivo.

Other names

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