Drug intelligence / Profile preview

SR3677

Development stage
Preclinical
Lead developer
Scripps Research
Modality
Small Molecules
Administration
Ophthalmic, Topical
01

Overview

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.

Other names
N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamideSR 3677SR3677SR-3677SR 3677 dihydrochlorideSR3677 dihydrochlorideSR-3677 dihydrochloride
02

Targets

ROCK2 (Rho-associated coiled-coil containing protein kinase 2)

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