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]
-
ROCK Related Products (111)
Related Products (111)
-
Chloroxoquinoline
0 ImagesCat. No.: HY-W110138CAS No.: 23833-97-8Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer.
-
ROCK-IN-9
0 ImagesCat. No.: HY-156593CAS No.: 2643334-76-1ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses.
-
ROCK-IN-10
0 ImagesCat. No.: HY-10833CAS No.: 1038549-25-5ROCK-IN-10 (compound 50) is a potent ROCK inhibitor with IC50 values of 6 nM and 4 nM for ROCK1 and ROCK2, respectively. ROCK-IN-10 shows >100-fold selectivity against other kinases.
-
20:4 Lyso PI
0 ImagesCat. No.: HY-150187CAS No.: 1246430-04-520:4 Lyso PI acts as an activator of GPR55 and RhoA. 20:4 Lyso PI activates the GPR55-RhoA-ROCK pathway, thereby inducing morphological changes, cytoskeleton assembly, cell rounding and stress fiber formation. 20:4 Lyso PI can be used in research related to diseases such as those of the nervous system.
-
Centaureidin
0 ImagesCat. No.: HY-N10341CAS No.: 17313-52-9Centaureidin is an orally active IFN-promoter that can be isolated from Bidens pilosa with an EC50 of 0.9 μg/mL. Centaureidin activates the Rho signal pathway, leading to actin and tubulin disassembly, and resulting in dendrite retraction and stress fiber formation in melanocytes. Centaureidin shows high tumor cell growth inhibitory activities. Centaureidin significantly inhibits paw edema in mice[1][2][3][4][5].
-
Glycerophosphoinositol 4-phosphate
0 ImagesCat. No.: HY-171909CAS No.: 129830-96-2Synonyms: GroPIns-4-PGlycerophosphoinositol 4-phosphate (GroPIns-4-P) is a metabolite of phospholipase A and an inhibitor of adenylylcyclase. Glycerophosphoinositol 4-phosphate can regulate cAMP-dependent cellular functions. Glycerophosphoinositol 4-phosphate 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 can be used in research on cancer cell motility and invasiveness.
-
AR-13503 (Standard)
0 ImagesCat. No.: HY-12798CRCAS No.: 2309668-15-1Synonyms: AR-13324 M1 metabolite (Standard)Fluanisone (Standard) is the analytical standard of Fluanisone. This product is intended for research and analytical applications. Fluanisone has potent sedative effect in vivo. Fluanisone can be used to study schizophrenia.
-
ROCK-IN-D1
0 ImagesCat. No.: HY-123484CAS No.: 1219721-73-9ROCK-IN-D1 serves as a highly effective and selective inhibitor of ROCK.
-
(R)-AR-13503
0 ImagesSynonyms: (R)-AR-13324 M1 metabolite(R)-AR-13503 ((R)-AR-13324 M1 metabolite) is the the (R)-enantiomer of AR-13503 (HY-12798C). AR-13503 is the hydrolytic metabolite of AR-13324 mesylate. AR-13324 is a ROCK kinase and PKC inhibitor with anti-angiogenic and retinal health-improving effects, showing potential for use in retinal disease research.
-
(Rac)-NRL-1049 dihydrochloride
0 ImagesCat. No.: HY-162596ACAS No.: 863638-93-1Synonyms: (Rac)-BA-1049(Rac)-NRL-1049 is the racemic mixture of NRL-1049 (BA-1049 (free base)) (HY-162596). NRL-1049 is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations.
-
Bazipsudil
0 ImagesCat. No.: HY-187858CAS No.: 2292312-76-4Bazipsudil is a potent, selective Rho-associated protein kinase (ROCK) inhibitor.
-
CCG-232964
0 ImagesCat. No.: HY-130011CAS No.: 2349373-70-0CCG-232964 is an orally active inhibitor of Rho/MRTF/SRF. CCG-232964 inhibits LPA-induced CTGF gene expression.
-
WF-536
0 ImagesCat. No.: HY-118837CAS No.: 539857-64-2
-
ROCK-IN-11
0 ImagesCat. No.: HY-W295201CAS No.: 445267-51-6
-
3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine
0 ImagesCat. No.: HY-N12466CAS No.: 2226941-29-13′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) is an inhibitor of protein kinases, with IC50s of 0.092, 0.26, 0.77 μM for PKC-α, ROCK, ASK1. 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine shows potent cytotoxicity against PC-3 cancer cells with an IC50 value of 0.16 μM.
-
ROCK-IN-D2
0 ImagesCat. No.: HY-116238CAS No.: 1219721-78-4ROCK-IN-D2 is a potent and selective ROCK inhibitor.
