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Transglutaminase 2 (TG2), which mediates post‐translational modifications of multiple intracellular enzymes, is involved in the pathogenesis and progression of cancer. We used 1H‐NMR metabolomics to study the effects of AA9, a novel TG2 inhibitor, on two breast cancer cell lines with distinct phenotypes, MCF‐7 and MDA‐MB‐231. AA9 can promote apoptosis in both cell lines, but it is particularly effective...