ROCK
ROCK (Rho-associated coiled-coil containing protein kinase) is a major downstream effector of the small GTPase RhoA and functions as a central regulator of actomyosin contractility, cytoskeletal organization, cell adhesion, migration, proliferation, and gene expression[1][2]. ROCK signaling coordinates multiple biological processes through phosphorylation-dependent control of myosin phosphatase and other cytoskeletal regulators, thereby influencing cellular morphology, motility, and tissue remodeling[1][3]. Mechanistically, the ROCK pathway is closely linked to endothelial function, smooth muscle contraction, inflammatory responses, and angiogenic regulation, making it relevant to diverse physiological and pathological contexts[1][4]. In disease models, aberrant ROCK activity has been associated with cardiovascular disorders, vascular remodeling, neurodegenerative conditions, fibrosis, and cancer progression, where altered cytoskeletal dynamics and cell migration contribute to disease development[1][3][4]. Compared with related isoforms, ROCK1 and ROCK2 share high kinase-domain homology but exhibit distinct biological functions and regulatory properties, indicating nonredundant roles in cellular signaling networks[2]. ROCK1 is broadly associated with cytoskeletal regulation and cell motility, whereas ROCK2 has been implicated in immune regulation, T-cell plasticity, macrophage polarization, and tissue-specific signaling processes[2][5]. For experimental applications, pharmacological ROCK inhibition is widely used to investigate RhoA-dependent signaling, and inhibitors such as fasudil have demonstrated utility in models of vascular and neurodegenerative disease by suppressing excessive ROCK activity and modulating downstream cellular responses[4][6].
References:
- [1]. Shi J, et al. Rho kinases in cardiovascular physiology and pathophysiology: the effect of fasudil. J Cardiovasc Pharmacol. 2013 Oct;62(4):341-54. [Content Brief]
- [2]. Julian L, et al. Rho-associated coiled-coil containing kinases (ROCK): structure, regulation, and functions. Small GTPases. 2014;5:e29846. [Content Brief]
- [3]. Liu J, et al. Rho-Associated Coiled-Coil Kinase (ROCK) in Molecular Regulation of Angiogenesis. Theranostics. 2018 Nov 26;8(21):6053-6069. [Content Brief]
- [4]. Schofield AV, et al. Rho-associated coiled-coil kinase (ROCK) signaling and disease. Crit Rev Biochem Mol Biol. 2013 Jul-Aug;48(4):301-16. [Content Brief]
- [5]. Database: Guide to pharmacology.
- [6]. Ye Q, et al. Role of Rho-associated kinases and their inhibitor fasudil in neurodegenerative diseases. Front Neurosci. 2024 Nov 19;18:1481983. [Content Brief]
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ROCK Related Products (111)
Related Products (111)
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ROCK-IN-4
0 ImagesCat. No.: HY-151189CAS No.: 2488395-07-7ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. ROCK-IN-4 reversibly depolymerizes F-actin, and suppresses mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 can be used for glaucoma or ocular hypertension research.
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OXA-06
0 ImagesCat. No.: HY-110335ACAS No.: 944955-32-2OXA-06 is a pharmacologic inhibitor of ROCK, possessing antitumor activity by impairing cell migration and MYPT1 phosphorylation in PANC-1 cells.
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GKI-1 (Standard)
0 ImagesCat. No.: HY-100521RCAS No.: 2444764-03-6GKI-1 (Standard) is the analytical standard of GKI-1 (HY-100521). This product is intended for research and analytical applications. GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 μM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 μM, but only weakly affected PKA.
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Cotosudil hydrochloride
0 ImagesCat. No.: HY-137436ACAS No.: 1258832-72-2Cotosudil hydrochloride is a ROCK kinase inhibitor that can be used in studies on glaucoma or ocular hypertension.
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AS1892802 (Standard)
0 ImagesCat. No.: HY-108519RCAS No.: 928320-12-1AS1892802 (Standard) is the analytical standard of AS1892802 (HY-108519). This product is intended for research and analytical applications. AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain.
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Rho-Kinase-IN-1 (Standard)
0 ImagesRho-Kinase-IN-1 (Standard) is the analytical standard of Rho-Kinase-IN-1 (HY-100270). This product is intended for research and analytical applications. Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008.
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Cinnamyl Alcohol-d5
0 ImagesCat. No.: HY-Y0078SCAS No.: 1044940-87-5
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Thiazovivin (Standard)
0 ImagesCat. No.: HY-13257RCAS No.: 1226056-71-8Thiazovivin (Standard) is the analytical standard of Thiazovivin (HY-13257). This product is intended for research and analytical applications. Thiazovivin is a potent ROCK inhibitor, which can protect human embryonic stem cells. Thiazovivin improves the efficiency of iPSC generation.
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ROCK2-IN-2 (Standard)
0 ImagesCat. No.: HY-103620RCAS No.: 1995065-79-6ROCK2-IN-2 (Standard) is the analytical standard of ROCK2-IN-2 (HY-103620). This product is intended for research and analytical applications. ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM.
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RKi-1447 dihydrochloride (Standard)
0 ImagesCat. No.: HY-110339RCAS No.: 1782109-09-4RKi-1447 dihydrochloride (Standard) is the analytical standard of RKi-1447 (dihydrochloride) (HY-110339). This product is intended for research and analytical applications. RKi 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKi 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.
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CMPD101 (Standard)
0 ImagesCat. No.: HY-103045RCAS No.: 865608-11-3CMPD101 (Standard) is the analytical standard of CMPD101 (HY-103045). This product is intended for research and analytical applications. CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
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SB-772077B dihydrochloride (Standard)
0 ImagesCat. No.: HY-108518RCAS No.: 607373-46-6SB-772077B dihydrochloride (Standard) is the analytical standard of SB-772077B (dihydrochloride) (HY-108518). This product is intended for research and analytical applications. SB-772077B dihydrochloride is an orally active aminofuran-based Rho Kinase ((ROCK)) inhibitor with IC50 values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytoKines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases.
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Belumosudil mesylate (Standard)
0 ImagesSynonyms: KD025 mesylate (Standard); SLx-2119 mesylate (Standard)Belumosudil (mesylate) (Standard) is the analytical standard of Belumosudil (mesylate). This product is intended for research and analytical applications. Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
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Hydroxyfasudil hydrochloride (Standard)
0 ImagesCat. No.: HY-13911ARCAS No.: 155558-32-0Synonyms: HA-1100 hydrochloride (Standard); HA 1100 hydrochloride (Standard); HA1100 hydrochloride (Standard)Hydroxyfasudil (hydrochloride) (Standard) is the analytical standard of Hydroxyfasudil (hydrochloride). This product is intended for research and analytical applications. Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
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GSK429286A (Standard)
0 ImagesCat. No.: HY-11000RCAS No.: 864082-47-3GSK429286A (Standard) is the analytical standard of GSK429286A (HY-11000). This product is intended for research and analytical applications. GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
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8-iso Prostaglandin F1β
0 ImagesCat. No.: HY-130448CAS No.: 26771-95-98-iso Prostaglandin F1β is an isoprostane, that exhibits vasoconstrictive effect in neonatal porcine pulmonary arteries, pulmonary veins, and mesenteric arteries. 8-iso Prostaglandin F1β targets TXA2 receptor and exhibits the blood vessel contractile efficacy under the influence of tyrosine kinase and Rho kinase.
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Y-30141
0 ImagesCat. No.: HY-183451CAS No.: 199433-55-1Y-30141 is a hinge-binding 7-azaindole-based Rho kinase (ROCK) inhibitor. Y-30141 can be used for the research of hypertension.
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HA-100 (Standard)
0 ImagesCat. No.: HY-100984RCAS No.: 84468-24-6HA-100 (Standard) is the analytical standard of HA-100 (HY-100984). This product is intended for research and analytical applications. HA-100 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 also used as a ROCK inhibitor.
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BAY-549 (Standard)
0 ImagesCat. No.: HY-10319RCAS No.: 867017-68-3Synonyms: ROCK-IN-2 (Standard); Azaindole 1 (Standard); TC-S 7001 (Standard)BAY-549 (Standard) is the analytical standard of BAY-549 (HY-10319). This product is intended for research and analytical applications. BAY-549 (Azaindole 1), a chemical probe, is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively.
