ROCK inhibitor-2 is a selective Rho kinase (ROCK) inhibitor with IC50 values of 17nM and 2nM for ROCK1 and ROCK2, respectively, and has anti-tumor activity[1, 2]. ROCK is a serine/threonine protein kinase and a downstream target effector molecule of Rho. ROCK can regulate multiple functions such as cell contraction, migration, adhesion and proliferation[3, 4]. ROCK inhibitor-2 belongs to the aminopyridine class of compounds and is a structural analog of Y-27632[5]. ROCK inhibitor-2 may help improve vision loss and treat glaucoma[6].
In vitro, treatment of human osteosarcoma cell line (U2OS cells) with ROCK inhibitor-2 (50μM) for 48h significantly inhibited cell migration and invasion and caused mitochondrial dysfunction[2].
References:
[1]Feng Y, LoGrasso P V, Defert O, et al. Rho kinase (ROCK) inhibitors and their therapeutic potential[J]. Journal of medicinal chemistry, 2016, 59(6): 2269-2300.
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[3]Liu J, Wada Y, Katsura M, et al. Rho-associated coiled-coil kinase (ROCK) in molecular regulation of angiogenesis[J]. Theranostics, 2018, 8(21): 6053.
[4]Liao J K, Seto M, Noma K. Rho kinase (ROCK) inhibitors[J]. Journal of cardiovascular pharmacology, 2007, 50(1): 17-24.
[5]Shahin R, Shaheen O, El-Dahiyat F, et al. Research advances in kinase enzymes and inhibitors for cardiovascular disease treatment[J]. Future science OA, 2017, 3(4): FSO204.
[6]Abbhi V, Piplani P. Rho-kinase (ROCK) inhibitors-a neuroprotective therapeutic paradigm with a focus on ocular utility[J]. Current Medicinal Chemistry, 2020, 27(14): 2222-2256.