rhosin

Rhosin is a selective, small-molecule inhibitor of the RhoA GTPase. It functions by binding to the surface of RhoA and specifically disrupting its interaction with Rho-specific guanine nucleotide exchange factors (RhoGEFs), such as LARG, p115RhoGEF, and PDZ-RhoGEF. By preventing the exchange of GDP for GTP, Rhosin effectively blocks RhoA activation and its downstream signaling pathways, including the RhoA/ROCK axis. This inhibition modulates various cellular processes such as cytoskeletal remodeling, actomyosin contractility, and cell migration. Rhosin has been extensively utilized as a pharmacological tool in preclinical research to investigate the role of RhoA in diverse pathologies, including endothelial barrier dysfunction in acute lung injury, viral morphogenesis (e.g., RSV and HCMV), neurodevelopmental disorders associated with 16p11.2 deletion, and platelet activation. While it shows therapeutic potential in animal models for conditions like opioid dependence and thrombosis, it is currently primarily used as a research-use-only reagent.

Other names

rhosin hydrochloriderhosin chloride