ROCK2
ROCK2 (Rho-associated coiled-coil-containing protein kinase 2) is a serine/threonine kinase that functions as a major downstream effector of Rho GTPases and regulates cytokinesis, smooth muscle contraction, actin stress fiber formation, focal adhesion dynamics, and transcriptional responses linked to cytoskeletal remodeling[1][2]. Mechanistically, ROCK2 promotes actomyosin contractility through signaling networks that control actin organization, cell morphology, migration, proliferation, adhesion, and inflammatory responses, placing it at the center of cytoskeleton-dependent cellular regulation[3][5]. Because these processes govern tissue homeostasis and cellular adaptation, dysregulated ROCK signaling has been implicated in cardiovascular, neurodegenerative, inflammatory, and cancer-associated pathologies[3][2]. In experimental disease models, ROCK2 has been identified as an important regulator of neuronal survival, axonal stability after injury, and regenerative responses, supporting its utility for studying neurodegeneration and neural repair mechanisms[4]. Compared with the closely related isoform ROCK1, ROCK2 shares high homology within the kinase domain but exhibits distinct tissue distribution and isoform-specific biological functions, highlighting the importance of discriminating ROCK2-dependent signaling from broader ROCK activity in mechanistic studies[3][2]. For experimental applications, pharmacological inhibition of ROCK signaling is widely used to interrogate cytoskeletal regulation and disease-associated pathways, and the development of isoform-selective inhibitors has increased interest in defining ROCK2-specific functions with greater precision[2]>.
References:
- [1]. ROCK2 gene information from NCBI.
- [2]. Wikipedia.
- [3]. Julian L, et al. Rho-associated coiled-coil containing kinases (ROCK): structure, regulation, and functions. Small GTPases. 2014;5:e29846. [Content Brief]
- [4]. Wikipedia.
- [5]. Koch JC, et al. ROCK2 is a major regulator of axonal degeneration, neuronal death and axonal regeneration in the CNS. Cell Death Dis. 2014 May 15;5(5):e1225. [Content Brief]
- [6]. Loirand G. Rho Kinases in Health and Disease: From Basic Science to Translational Research. Pharmacol Rev. 2015;67(4):1074-1095.
All Product Categories
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ROCK2 Related Products (76)
Related Products (76)
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Antibodies (1)
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ROCK2-IN-19
0 ImagesCat. No.: HY-189083ROCK2-IN-19, the non-isotopic form of compound 22d, is an orally active and selective ROCK2 inhibitor with an IC50 value of 13 nM. ROCK2-IN-19 selectively inhibits the phosphorylation of STAT3 at tyrosine 705, and suppresses breast cancer metastasis by disrupting the ROCK2-STAT3 signaling axis. ROCK2-IN-19 exhibits anti-metastatic activity in both cancer cells and xenograft models. ROCK2-IN-19 can be used in breast cancer-related research.
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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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ROCK2-IN-5
0 ImagesCat. No.: HY-145294CAS No.: 3031515-48-4ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation.
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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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RX-044
0 ImagesCat. No.: HY-187204RX-044 is a ROCK1/ROCK2 inhibitor with ROCK1 IC50 10.01 nM and ROCK2 IC50 9.68 nM, and demonstrates kinase selectivity. RX-044 induces reversible cell retraction, modulates cytoskeletal organization via F-actin depolymerization, inhibits cell contractility, and attenuates TGF-β2-induced cell migration. RX-044 preserves retinal ganglion cell survival, restores electroretinography responses, and ameliorates histopathological changes. RX-044 lowers intraocular pressure in a mouse ocular hypertension model. RX-044 shows no cytotoxicity in target cells. RX-044 exhibits initial ocular irritation that subsides with extended dosing. RX-044 can be used for the research of glaucoma.
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ROCK2-IN-14
0 ImagesCat. No.: HY-181576CAS No.: 3115784-59-0ROCK2-IN-14 is an orally active, selective ROCK2 inhibitor (IC50=4.8 nM) with 212-fold selectivity over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 downregulates S100A9 expression, inhibits NM2 phosphorylation and restores cytoskeletal abnormalities. Furthermore, ROCK2-IN-14 reduces inflammatory cytokine levels, alleviates skin inflammation and exerts anti-inflammatory activity. ROCK2-IN-14 also significantly inhibits ear thickening in a mouse model of atopic dermatitis (AD), and decreases the levels of IgE, TNF-α, IL-6 and TSLP. ROCK2-IN-14 can be used for research on atopic dermatitis.
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ROCK-IN-6
0 ImagesCat. No.: HY-153564CAS No.: 2489328-74-5
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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-N15301ANocarnickelamide 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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CMPD101 hydrochloride
0 ImagesCat. No.: HY-103045ACAS No.: 1941168-71-3CMPD101 hydrochloride is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM, respectively. CMPD101 hydrochloride also inhibits Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s =1.4 μM and 8.1 μM, respectively).
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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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ROCK-IN-18
0 ImagesCat. No.: HY-188017CAS No.: 3060895-25-9ROCK-IN-18 is a blood-brain barrier-permeable selective inhibitor of the ROCK2 protein kinase. ROCK-IN-18 is applicable to research related to cardiovascular diseases, neurological diseases, breast cancer, colon cancer, pancreatic cancer and other disorders.
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ROCK-IN-13
0 ImagesCat. No.: HY-116233CAS No.: 1219727-16-8ROCK-IN-13 is a ROCK2 inhibitor with an IC50 of 8 nM against human ROCK2. ROCK-IN-13 has the potential for use in the research of diseases such as multiple sclerosis, glaucoma, and cardiovascular diseases.
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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.
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LX7101 monohydrochloride
0 ImagesCat. No.: HY-12659BCAS No.: 2319882-48-7LX7101 monohydrochloride is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 monohydrochloride proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 monohydrochloride has the potential for ocular hypertension and associated glaucoma research.
