GK921

GK921 is a **small-molecule transglutaminase 2 inhibitor** developed as a preclinical research compound for oncology. It inhibits **transglutaminase 2** activity, with published and catalog data describing micromolar potency against recombinant human TGase 2, and mechanistic literature indicating binding to an **allosteric N-terminal region** of the enzyme rather than the catalytic active site. In cancer models, especially renal cell carcinoma and pancreatic adenocarcinoma, GK921 has been reported to suppress TGase 2 driven signaling, stabilize **p53**, inhibit epithelial-to-mesenchymal transition, and enhance apoptosis; it has also shown combination activity with cisplatin in pancreatic cancer models. The available evidence supports GK921 as an **investigational preclinical antineoplastic targeted small molecule** rather than an approved medicine, and a specific commercial developer is not clearly established from the provided source context.