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 (60)
Related Products (60)
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Antibodies (1)
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Fasudil dihydrochloride
0 ImagesSynonyms: HA-1077 dihydrochloride; AT-877 dihydrochlorideFasudil (HA-1077; AT877) dihydrochloride 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 dihydrochloride is also a potent Ca2+ channel antagonist and vasodilator.
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ROCK2-IN-12
0 ImagesROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0 nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research.
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β-Patchoulene
0 Imagesβ-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. β-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. β-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. β-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma.
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Hu7691 free base
0 ImagesCat. No.: HY-132302ACAS No.: 2241232-43-7
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ROCK/HDAC-IN-2
0 ImagesCat. No.: HY-172177ROCK/HDAC-IN-2 (Compound C-9) is a ROCK/HDAC inhibitor, with IC50 values of 0.185 µM, 0.8 µM, and 0.7 µM for HDAC6, ROCK1, and ROCK2, respectively. ROCK/HDAC-IN-2 can induce apoptosis and changes in mitochondrial membrane potential in cancer cells, demonstrating significant antitumor activity. ROCK/HDAC-IN-2 can be used in the research of pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).
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Fasudil hydrochloride semihydrate
0 ImagesCat. No.: HY-10341BCAS No.: 186694-02-0Synonyms: HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrateFasudil (HA-1077; AT877) hydrochloride semihydrate 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 semihydrate is also a potent Ca2+ channel antagonist and vasodilator.
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ROCK/HDAC-IN-1
0 ImagesCat. No.: HY-168650ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity.
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Verosudil hydrochloride
0 ImagesCat. No.: HY-16758ACAS No.: 1414854-44-6Synonyms: AR-12286 hydrochlorideVerosudil (AR-12286) hydrochloride is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is a ROCK inhibitor. Verosudil hydrochloride has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil hydrochloride is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil hydrochloride increases trabecular outflow capacity to reduce intraocular pressure. Verosudil hydrochloride is useful in the study of glaucoma and ocular hypertension.
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LASSBio-2382
0 ImagesCat. No.: HY-181582CAS No.: 2487752-24-7
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SR-3677 dihydrochloride
0 ImagesCat. No.: HY-13300ACAS No.: 1781628-88-3SR-3677 dihydrochloride (compound 5) is a potent and selective ROCK-I and ROCK-II inhibitor with an IC50 values of 56 nM and 3 nM.
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5-Nitro-1H-indazole-3-carbonitrile
0 ImagesCat. No.: HY-W047432CAS No.: 90348-29-1Synonyms: DL08055-Nitro-1H-indazole-3-carbonitrile (DL0805) is a Rho kinase(ROCK) inhibitor with an IC50 of 6.67 μM for ROCK-I. 5-Nitro-1H-indazole-3-carbonitrile reduces Norepinephrine (HY-13715)-induced transient contraction and inhibits contraction induced by increasing external calcium in the endothelium-denuded rings of rat models. 5-Nitro-1H-indazole-3-carbonitrile has a vasorelaxant activity but high toxicity. 5-Nitro-1H-indazole-3-carbonitrile can be used for cardiovascular diseases, especially hypertension research.
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LASSBio-2389
0 ImagesCat. No.: HY-181583CAS No.: 2671377-38-9LASSBio-2389 is a selective ROCK2 inhibitor with an IC50 of 0.051 μM and an IC50 of 1.143 μM against ROCK1. LASSBio-2389 reduces the viability of MDA-MB-231 cells and inhibits cell migration. LASSBio-2389 is applicable to the research of triple-negative breast cancer.
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ROCK2-IN-10
0 ImagesCat. No.: HY-175843ROCK2-IN-10 is a potent and selective ROCK2 inhibitor (IC50 = 0.020 μM) with 41-fold selectivity over isoform ROCK1. ROCK2-IN-10 inhibits metastasis by disrupting the cytoskeleton, independent of proliferative suppression. ROCK2-IN-10 shows superior inhibitory potency against cancer cell metastasis, which closely related to the suppression of STAT3 phosphorylation. ROCK2-IN-10 can be used for breast cancer metastasis research.
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Nocarnickelamide B TFA
0 ImagesCat. No.: HY-N15301APurity: 99.82%Nocarnickelamide B TFA is a ROCK1/2 inhibitor with IC50 values of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B TFA inhibits the activation of ROCK-regulated cytoskeletal contraction markers (especially myosin light chain) in human trabecular meshwork cells. Nocarnickelamide B TFA can be used in the research of glaucoma.
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JAK1/3-IN-1
0 ImagesCat. No.: HY-123939CAS No.: 1400687-19-5JAK1/3-IN-1 is a selective, orally active JAK1/3 inhibitor with IC50 values of 1.9 nM and 0.9 nM, respectively. JAK1/3-IN-1 significantly reduces the mean arterial blood pressure and significantly increases the heart rate in rabbits. JAK1/3-IN-1 decreases the mean arterial blood pressure in conscious telemetered rats and induces lethal cardiovascular effects.
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Nocarnickelamide B
0 ImagesCat. No.: HY-N15301Nocarnickelamide B (Compound 2) is a linear peptide and ROCK1/2 inhibitor. Nocarnickelamide B exhibits dual inhibitory activity against ROCK1 and ROCK2 with IC50s of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B binds to the ATP-binding site. Nocarnickelamide B inhibits the activation of ROCK-regulated cytoskeletal contraction markers such as the myosin light chain. Nocarnickelamide B is potential for glaucoma reasearch.
