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 (109)
Related Products (109)
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Coptisine Sulfate
0 ImagesCoptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease.
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CAY10746
0 ImagesCAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR).
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(rac)-AR-13503
0 ImagesSynonyms: (rac)-AR-13324 M1 metabolite(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice.
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RhoA-ROCK-IN-1
0 ImagesRhoA-ROCK-IN-1 (Compound b19) is an inhibitor of RhoA/ROCK. RhoA-ROCK-IN-1 can significantly inhibit cell proliferation, migration, and invasion, while promoting cell apoptosis. RhoA-ROCK-IN-1 demonstrates remarkable anticancer activity by inhibiting the RhoA/ROCK pathway.
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Cotosudil
0 ImagesCotosudil is a ROCK kinase inhibitor, which can be used for glaucoma or ocular hypertension research.
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Scaff10-8
0 ImagesScaff10-8 is a RhoA inhibitor. Scaff10-8 binds to RhoA, inhibits AKAP-Lbc-mediated RhoA activation. Scaff10-8 can be used for research on diabetes insipidus and bipolar disorder.
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OXA-06 hydrochloride
0 ImagesOXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis.
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NRL-1049 dihydrochloride
0 ImagesSynonyms: BA-1049NRL-1049 dihydrochloride (BA-1049) is a selective and orally active rho-associated protein kinase 2 (ROCK2) inhibitor with an IC50 of 0.59 μM. NRL-1049 dihydrochloride shows selectivity for ROCK2 is 44 times that of ROCK1 (IC50 = 26 μM). NRL-1049 dihydrochloride can preserve the blood-brain barrier after acute injury.
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Y-27632 hydrochloride hydrate
0 ImagesY-27632 hydrochloride hydrate is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 hydrochloride hydrate exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 hydrochloride hydrate enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 hydrochloride hydrate induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 hydrochloride hydrate promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
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AS1892802
0 ImagesAS1892802 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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PT-262
0 ImagesPT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity.
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Exoenzyme C3, clostridium botulinum
0 ImagesCat. No.: HY-P2325CAS No.: 58319-92-9Exoenzyme C3, clostridium botulinum, is a mono-ADP-ribosylating enzyme. Exoenzyme C3, clostridium botulinum specifically modifies RhoA, B, and C by transferring ADP-ribose to them, thereby inactivating these GTPases. Exoenzyme C3, clostridium botulinum can induce neuronal axonal and dendritic growth, inhibit macrophage migration, and regulate cytoskeletal dynamics. Exoenzyme C3, clostridium botulinum can be used in the research of spinal cord injury and diabetic painful neuropathy.
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Palmitoyl 3-carbacyclic phosphatidic acid
0 ImagesPalmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model.
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Rho-Kinase-IN-3
0 ImagesRho-Kinase-IN-3 (compound 12) is a potent and selective Rho kinase (ROCK1) inhibitor with an IC50 value of 8 nM. Rho-Kinase-IN-3 can be used in research of hypertension.
