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Description: GK921 is a novel and potent inhibitor of transglutaminase 2 (TGase) with an IC50 of 7.71 uM for human recombinant TGase 2. GK921 showed cytotoxicity to RCC (average GI50 in eight RCC cell lines: 0.905 uM). A single treatment with GK921 almost completely reduced tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models. TGase 2 inhibitor GK921 abrogates RCC growth in xenograft tumor models, suggesting the possibility of a new therapeutic approach to RCC.
References: J Cancer Res Clin Oncol. 2014 May; 140(5):757-67.
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