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HA-1077 dihydrochloride has been shown to be a vasodilating agent as well as a potent inhibitor of Rock-2 (Rho-associated Kinase II), cGKI (cGMP-dependent protein kinase), PKA (cAMP-dependent protein kinase), MYLK, and CaMKII. Rho kinase signaling pathways are thought to cause invasion, migration, and proliferation of certain cells. Studies have shown this compound can also inhibit myosin light chain kinase in vitro and suppress cell rounding by myosin light chain phosphorylation. Mechanistic experiments report that HA-1077 inhibits vascular smooth muscle contraction by acting as a calcium channel protein inhibitor. HA-1077 dihydrochloride is an inhibitor of MSK1, PKC, PRK2 and Rsk-2.
Wickman, G., C. Lan.; and B. Vollrath. Functional roles of the rho/rho kinase pathway and protein kinase C in the regulation of cerebrovascular constriction mediated by hemoglobin: relevance to subarachnoid hemorrhage and vasospasm. Circ Res. 201292 (7), 809-16.