ROCK inhibitor-2

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.
[1] Zhang W, Zhao W, Li Q, et al. 3D-printing magnesium–polycaprolactone loaded with melatonin inhibits the development of osteosarcoma by regulating cell-in-cell structures[J]. Journal of Nanobiotechnology, 2021, 19: 1-20.
[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.

ROCK inhibitor-2是一种选择性Rho激酶（ROCK）抑制剂，抑制ROCK1和ROCK2的IC₅₀值分别为17nM和2nM，具有抗肿瘤活性^{[1, 2]}。ROCK是丝氨酸/苏氨酸蛋白激酶，属于Rho下游靶效应分子，能够调节细胞收缩、迁移、黏附和增殖等多种功能^{[3, 4]}。ROCK inhibitor-2属于氨基吡啶类化合物，是Y-27632的结构类似物^[5]。ROCK inhibitor-2可能有助于改善视力丧失，治疗青光眼^[6]。

在体外，ROCK inhibitor-2（50μM）处理人骨肉瘤细胞系（U2OS细胞）48h，显著抑制了细胞迁移和侵袭，并导致线粒体功能障碍^[2]。