ZGDHu-1

ZGDHu-1 is a **novel small molecule tetrazine compound** with demonstrated antitumor activity in preclinical studies. Originally synthesized and patented by Professor Wei-Xiao Hu at the College of Pharmaceutical Science, Zhejiang University of Technology (China), ZGDHu-1 acts as a **proteasome inhibitor** and has been shown to induce apoptosis and cell cycle arrest (specifically G2/M phase) in several cancer cell lines, including Kasumi-1 acute myeloid leukemia cells, CLL (chronic lymphocytic leukemia) cells, mantle cell lymphoma cells, and others. Preclinical research indicates that ZGDHu-1's anticancer effects involve upregulation of pro-apoptotic proteins (such as Bax, p53, and Fas), downregulation of anti-apoptotic Bcl-2, increased reactive oxygen species (ROS) generation, and dysregulation of mitochondrial membrane potential. ZGDHu-1 selectively inhibits cancer cells over normal cells in vitro, and has shown low toxicity in animal models. The precise molecular targets in the proteasome or ancillary pathways are still under investigation. ZGDHu-1 is investigational and has not reached clinical approval.

Other names

N,N′-di-(m-methylphenyl)-3,6-dimethyl-1,4-dihydro-1,2,4,5-tetrazine-1,4-dicarboamide