EHop-167

EHop-167 (also known as MBQ-167) is a potent, small-molecule dual inhibitor of the Rho GTPases Rac and Cdc42. Developed as an improved derivative of EHop-016, EHop-167 inhibits Rac and Cdc42 activity in the nanomolar range. By blocking these homologous GTPases, the drug disrupts downstream p21-activated kinase (PAK) signaling, which is critical for cytoskeletal organization, cell polarity, and cell migration. In metastatic breast cancer cells, treatment with EHop-167 leads to a loss of cell polarity, cell rounding, detachment from the extracellular matrix, and ultimately cell death via anoikis. Preclinical studies in mouse models of breast cancer have shown that EHop-167 significantly reduces tumor growth and prevents metastasis without causing significant systemic toxicity.

Other names

9-ethyl-3-(5-phenyl-1H-1,2,3-triazol-1-yl)-9H-carbazole