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Drug intelligence / Profile preview
SR3677 is a potent, highly selective, and ATP-competitive inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2), with an IC50 of approximately 3 nM. It exhibits high selectivity over ROCK1 (IC50 of ~56 nM) and other kinases. Discovered by researchers at the Scripps Research Institute, SR3677 has been investigated in preclinical models for the treatment of glaucoma, where it increases aqueous humor outflow, and Alzheimer's disease, where it suppresses amyloid-beta production by blocking ROCK2-mediated phosphorylation of amyloid precursor protein (APP). It is also widely used as a research tool to study Rho kinase signaling and smooth muscle contraction.
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