KCC009

KCC009 (also known as ERW1095B) is a small molecule, active-site-directed irreversible inhibitor of transglutaminase 2 (TG2, also known as tissue transglutaminase). Developed at Stanford University, KCC009 acts by covalently modifying the active-site cysteine residue of TG2, thereby blocking its transamidating activity. It has been extensively utilized as a preclinical research tool to investigate the role of TG2 in various pathological conditions, including celiac disease, neurodegenerative disorders (such as Parkinson's disease), and several cancers (such as glioblastoma, lung adenocarcinoma, and ovarian cancer). In oncology models, KCC009 disrupts fibronectin assembly in the extracellular matrix, impairs cell survival signaling pathways (such as Akt and NF-κB), and sensitizes tumor cells to chemotherapy and radiation therapy.

Other names

N-[(1S)-2-[[(3-bromo-4,5-dihydro-5-isoxazolyl)methyl]amino]-1-[(4-hydroxyphenyl)methyl]-2-oxoethyl]-carbamic acid, phenylmethyl ester