hTG2 inhibitor VA4 (VA4)

VA4 is a novel irreversible TG2 transamidase site-specific inhibitor.

hTG2 inhibitor VA4 (compound VA4) is an irreversible Type 2 transglutaminase (TG2) inhibitor. hTG2 inhibitor VA4 reacts exclusively at the TG2 transamidase site, inhibits both transamidase and GTP-binding activities[1].

[1] Kerr C, et al. Transamidase site-targeted agents alter the conformation of the transglutaminase cancer stem cell survival protein to reduce GTP binding activity and cancer stem cell survival. Oncogene. 2017 May 25;36(21):2981-2990. DOI:10.1038/onc.2016.452