ROCK1
ROCK1 is a RhoA effector serine/threonine kinase that regulates actomyosin cytoskeleton organization, smooth-muscle contraction, cell migration, and cell-shape control[1][2]. Mechanistically, ROCK1 promotes myosin light-chain phosphorylation and actomyosin contractility, and caspase-3 cleavage converts ROCK1 into an active apoptotic effector that drives membrane blebbing[3]. In vivo, ROCK1-deficient mice show failed eyelid and ventral body-wall closure, supporting its role in epithelial morphogenesis and actomyosin bundle assembly[4]. ROCK1 also regulates Beclin1-mediated autophagy, linking ROCK1 signaling to the balance between apoptosis and autophagy[8]. Compared with ROCK2, ROCK1 shows isoform-specific biology: ROCK1 destabilizes stress fibers through MLC2 phosphorylation and peripheral actomyosin contraction, whereas ROCK2 stabilizes actin through cofilin phosphorylation[5]. In glioblastoma models, ROCK1 is upregulated relative to normal brain tissue, and ROCK1 knockdown reduces proliferation and alters substrate-dependent migration, while ROCK2 knockdown produces different migration and proliferation effects[6]. For experimental applications, ROCK inhibitors provide tools to test ROCK-dependent contraction, motility, invasion, glaucoma, asthma, cancer, and cardiovascular mechanisms, although many compounds inhibit both ROCK1 and ROCK2[7].
References:
- [1]. Julian L, et al. Rho-associated coiled-coil containing kinases (ROCK): structure, regulation, and functions. Small GTPases. 2014;5:e29846. [Content Brief]
- [2]. Riento K, et al. Rocks: multifunctional kinases in cell behaviour. Nat Rev Mol Cell Biol. 2003 Jun;4(6):446-56. [Content Brief]
- [3]. Sebbagh M, et al. Caspase-3-mediated cleavage of ROCK I induces MLC phosphorylation and apoptotic membrane blebbing. Nat Cell Biol. 2001 Apr;3(4):346-52. [Content Brief]
- [4]. Shimizu Y, et al. ROCK-I regulates closure of the eyelids and ventral body wall by inducing assembly of actomyosin bundles. J Cell Biol. 2005 Mar 14;168(6):941-53. [Content Brief]
- [5]. Shi J, et al. Distinct roles for ROCK1 and ROCK2 in the regulation of cell detachment. Cell Death Dis. 2013 Feb 7;4(2):e483. [Content Brief]
- [6]. Mertsch S, et al. Opposing signaling of ROCK1 and ROCK2 determines the switching of substrate specificity and the mode of migration of glioblastoma cells. Mol Neurobiol. 2014 Apr;49(2):900-15. [Content Brief]
- [7]. Feng Y, et al. Rho Kinase (ROCK) Inhibitors and Their Therapeutic Potential. J Med Chem. 2016 Mar 24;59(6):2269-300. [Content Brief]
- [8]. Gurkar AU, et al. Identification of ROCK1 kinase as a critical regulator of Beclin1-mediated autophagy during metabolic stress. Nat Commun. 2013;4:2189. [Content Brief]
All Product Categories
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ROCK1 Related Products (57)
Related Products (57)
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Antibodies (1)
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Y-27632
0 ImagesY-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
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Fasudil Hydrochloride
0 ImagesSynonyms: HA-1077 Hydrochloride; AT-877 HydrochlorideFasudil (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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LASSBio-2389
0 ImagesCat. No.: HY-181583CAS No.: 2671377-38-9
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Fasudil
0 ImagesSynonyms: HA-1077; AT877Fasudil (HA-1077; AT877) 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 is also a potent Ca2+ channel antagonist and vasodilator.
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SB-772077B dihydrochloride
0 ImagesSB-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.
