ROCK

Hu7691 是一种具有口服活性、选择性和高效性的 Akt 抑制剂，抑制 Akt1、Akt2 和 Akt3，抑制神经母细胞瘤细胞增殖，诱导神经母细胞瘤细胞的分化。

ROCK-IN-2 (Azaindole 1) 是一种选择性，ATP-竞争型的ROCK 抑制剂，对ROCK-1和ROCK-2的IC50值分别为 0.6 和 1.1 nM。

CCG-222740 是一种口服有效的选择性Rho/MRTF 途径抑制剂。它也是 α-平滑肌的肌动蛋白表达抑制剂，可减少皮肤纤维化并阻止黑色素瘤转移。

ROCK-IN-32 is an effective Rho-kinase inhibitor.

WF-536 Hydrochloride, a novel inhibitor of ROCK, inhibits tumour metastasis in some animal models.

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

LX7101是 LIMK 和ROCK2高效抑制剂，对LIMK1/2、ROCK、PKA 的IC50分别为24、1.6、10 和小于1 nM。

GSK269962A (GSK269962A HCl) 是一种有效的ROCK 抑制剂，具有抗炎和血管舒张作用。它作用于重组人ROCK1和ROCK2，IC50分别为 1.6 和 4 nM。

GSK269962A hydrochloride (GSK 269962 hydrochloride) 是一种具有高效性和选择性的 ROCK 抑制剂，具有抗炎和血管舒张作用，抑制 ROCK1 和 ROCK2，可用于研究急性髓系白血病。

ROCK2-IN-6 hydrochloride (Comp A)为一种选择性ROCK2抑制剂，适用于研究ROCK介导的疾病、自身免疫性病症与炎症。

HA-100 是蛋白激酶和ROCK 抑制剂，抑制PKG，PKA，PKC 和MLC 激酶的IC50值分别为 4、8、12 和 240 μM。

RKI1313 (RKI-1313) 是一种选择性抑制剂，可抑制 ROCK 依赖性信号传导、细胞骨架变化、不依赖锚定的集落形成、迁移和侵袭。

Chroman 1 是高效的的ROCK 选择性抑制剂，对 ROCK2 (IC50=1 pM) 的抑制作用强于 ROCK1 (IC50=52 pM) 。它对MRCK 也有抑制作用，IC50为 150 nM。

Potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively). Feng et al (2008) Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors. J.Med.Chem. 51 6642 PMID:18834107

Zelasudil (RXC007) 是一种 Rho 相关 (ROCK) 激酶 抑制剂，可用于研究特发性肺纤维化和炎症。