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VA4 is a novel irreversible TG2 transamidase site-specific inhibitor. | [Uses]
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]. | [References]
[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 |
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