BIPM is a potent inhibitor of Rho-associated protein kinase 2 (ROCK2). Exposure of SH-SY5Y cells to BIPM led to significant changes in cell migration, actin stress fibers and neurite length. BIPM significantly inhibits phosphorylation of cofilin, a regula
Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK), which can penetrate the central nervous system (CNS). It exhibits a high affinity for ROCK2 with an inhibition constant (IC50) of 3 nM. This compound is of potential interest for further investigations in the field of Huntington's disease research [1].
LX7101 is a potent inhibitor of both LIM kinase (LIMK) 1 and 2, and Rho-associated kinase 1 (ROCK1) and ROCK2, with IC50 values of 32, 4.3, 69, and 32 nM, respectively. It is selective, demonstrated by its lack of cross-reactivity in a panel of binding assays involving 78 receptors, transporters, and an additional 430 kinases, at a concentration of 10 μM. The topical administration of LX7101 (3 μl of a 1 mg ml solution) to the eye has been shown to reduce intraocular pressure in a dexamethasone-induced mouse model of glaucoma.
Nocarnickelamides B (Compound 2) 是一种线性肽类ROCK1 2抑制剂,对ROCK1和ROCK2的IC50值分别为14.9 μM和21.9 μM。其通过结合于ATP结合位点发挥作用,抑制ROCK调控的细胞骨架收缩标志物(如肌球蛋白轻链的激活)。Nocarnickelamides B 在青光眼研究中具备应用潜力。