Ehop-016

Ehop-016 is a small molecule inhibitor of the Rho GTPases Rac1 and Cdc42, developed by researchers at the University of Puerto Rico. It acts by inhibiting the activation of these homologous proteins, which are frequently overexpressed in various cancers and play critical roles in regulating tumorigenesis, angiogenesis, invasion, and metastasis. Preclinical studies have demonstrated that Ehop-016 can significantly reduce cell viability and inhibit metastasis in models of triple-negative breast cancer (TNBC), gastric cancer, and pancreatic cancer. Furthermore, Ehop-016 has been shown to sensitize pancreatic cancer cells to gamma-irradiation by blocking the activation of the ATM/Chk2 and ATR/Chk1 pathways, thereby abrogating the radiation-induced G2/M checkpoint and delaying DNA double-strand break repair.