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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Fasudil Hydrochloride (Standard)
0 ImagesSynonyms: HA-1077 Hydrochloride (Standard); AT-877 Hydrochloride (Standard)Fasudil (Hydrochloride) (Standard) is the analytical standard of Fasudil (Hydrochloride). This product is intended for research and analytical applications. Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca2+ channel antagonist and vasodilator.
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Fasudil mesylate
0 ImagesCat. No.: HY-10341DCAS No.: 1001206-62-7Synonyms: HA-1077 mesylate; AT-877 mesylateFasudil (HA-1077; AT877) mesylate is a nonspecific and orally active RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil mesylate is also a potent Ca2+ channel antagonist and vasodilator.
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GSK317354A
0 ImagesCat. No.: HY-111239CAS No.: 874119-13-8GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research.
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HA-100 hydrochloride
0 ImagesCat. No.: HY-100984ACAS No.: 141543-63-7
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Rhodblock 1a
0 ImagesCat. No.: HY-134913CAS No.: 701226-08-6Rhodblock 1a is an inhibitor of the Rho kinase signaling pathway. It inhibits the normal formation of the cleavage furrow during cell division by interfering with the localization and function of Rho pathway proteins, causing some cells to fail to form a cleavage furrow or the formed cleavage furrow to break, resulting in binucleated cells. Rhodblock 1a can be used to study the mechanism of cell division and is expected to be used in the research of diseases such as cardiovascular diseases and cancer.
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Narciclasine (Standard)
0 ImagesCat. No.: HY-16563RCAS No.: 29477-83-6Synonyms: Lycoricidinol (Standard)Narciclasine (Standard) is the analytical standard of Narciclasine. This product is intended for research and analytical applications. Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
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BIPM
0 ImagesCat. No.: HY-100460CAS No.: 1070424-33-7
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Khasianine (Standard)
0 ImagesCat. No.: HY-N2322RCAS No.: 32449-98-2Khasianine (Standard) is the analytical standard of Khasianine (HY-N2322). This product is intended for research and analytical applications. Khasianine is a steroidal glycoalkaloid. Khasianine alleviates psoriasis-like skin inflammation by inhibiting the TNF-α/NF-κB axis. Khasianine can downregulate the RhoA pathway and exhibits potential antimetastatic activity. Khasianine upregulates the expression of TNFR I and TNFR II without inducing apoptotic effects. Khasianine can be used in studies related to psoriasis, pancreatic ductal adenocarcinoma, and liver cancer.
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Glycerophosphoinositol 4-phosphate disodium
0 ImagesCat. No.: HY-171909ASynonyms: GroPIns-4-P disodiumGlycerophosphoinositol 4-phosphate (GroPIns-4-P) disodium is a metabolite of phospholipase A and an inhibitor of adenylylcyclase. Glycerophosphoinositol 4-phosphate disodium can regulate cAMP-dependent cellular functions. Glycerophosphoinositol 4-phosphate disodium can also induce the formation of membrane ruffles and stress fibers in serum-starved Swiss 3T3 cells by activating the small GTPases Rac and Rho, respectively. Glycerophosphoinositol 4-phosphate disodium can be used in research on cancer cell motility and invasiveness.
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Y-27632-d4 hydrochloride hydrate
0 ImagesCat. No.: HY-W700452Y-27632-d4 hydrochloride hydrate is the deuterium labeled Y-27632 hydrochloride hydrate (HY-10071A). Y-27632 hydrochloride hydrate is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 hydrochloride hydrate attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 hydrochloride hydrate also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 hydrochloride hydrate primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
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Fimosudil
0 ImagesCat. No.: HY-156592CAS No.: 2260506-59-8Synonyms: ROCK2-IN-6Fimosudil (ROCK2-IN-6) (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research.
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Y-33075 hydrochloride
0 ImagesCat. No.: HY-10068CAS No.: 471843-75-1Synonyms: Y-39983Y-33075 hydrochloride (Y-39983) is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.
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ROCK-IN-32
0 ImagesCat. No.: HY-113641CAS No.: 1013117-40-2ROCK-IN-32 is a ROCK inhibitor, with an IC50 value of 11 nM for ROCK2. ROCK-IN-32 can be used in research of cardiovascular disease, cancer and inflammation.
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1-Oleoyl lysophosphatidic acid sodium (GMP)
0 ImagesCat. No.: HY-107614GCAS No.: 325465-93-8Synonyms: 1-Oleoyl-sn-glycero-3-phosphate sodium (GMP); 1-Oleoyl-LPA sodium (GMP)1-Oleoyl lysophosphatidic acid sodium (GMP) is the GMP-grade form of 1-Oleoyl lysophosphatidic acid sodium (HY-107614). GMP-grade small molecules serve as auxiliary reagents in cell therapy. 1-Oleoyl lysophosphatidic acid sodium is a bioactive lipid signaling molecule. 1-Oleoyl lysophosphatidic acid sodium inhibits lysoPLD-catalyzed hydrolysis of lysophosphatidylcholine and FS-3. 1-Oleoyl lysophosphatidic acid sodium activates LPA1 and LPA2, thereby triggering calcium mobilization, NFATc1 translocation, Rho/ROCK activation, Smad2/3 phosphorylation and c-Fos expression. 1-Oleoyl lysophosphatidic acid sodium induces anxiety-like, depression-like and hypoactivity phenotypes, regulates osteoclast cytoskeleton and viability, reduces osteoclast bone resorptive activity, and drives mesenchymal stem cell differentiation into myofibroblast-like cells. 1-Oleoyl lysophosphatidic acid sodium stimulates the secretion of transforming growth factor-β1 and stromal cell-derived factor-1. 1-Oleoyl lysophosphatidic acid sodium is applicable to research related to anxiety, depression and ovarian cancer.
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ROCK-IN-7
0 ImagesCat. No.: HY-153569CAS No.: 2376635-95-7
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4-(Indolin-1-yl)pyrimidin-2-amine
0 ImagesCat. No.: HY-W1058961CAS No.: 1401661-20-84-(Indolin-1-yl) pyrimidin-2-amine (13a, non-salt form) is a ROCK inhibitor.
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ROCK-IN-8
0 ImagesCat. No.: HY-156550CAS No.: 1621103-79-4ROCK-IN-8 (Example 4) is a ROCK inhibitor, with an IC50 value less than 100 nM. ROCK-IN-8 has anti-inflammatory activity. ROCK-IN-8 can be used for research of respiratory and gastro-intestinal diseases.
