2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Cytoskeleton
    Stem Cell/Wnt
    TGF-beta/Smad
  4. ROCK

ROCK

Rho-associated protein kinase; Rho-associated kinase; Rho-kinase; ROK

ROCK

Related Products

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ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. ROCKs (ROCK1 and ROCK2) occur in mammals, zebrafish, Xenopus, invertebrates and chicken. Human ROCK1 has a molecular mass of 158 kDa and is a major downstream effector of the small GTPase RhoA. Mammalian ROCK consists of a kinase domain, acoiled-coil region and a Pleckstrin homology (PH) domain, which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular fold if RhoA-GTP is not present. ROCK plays a role in a wide range of different cellular phenomena, as ROCK is a downstream effector protein of the small GTPase Rho, which is one of the major regulators of the cytoskeleton.

ROCK Isoform Specific Products:

ROCK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-123484
    ROCK-IN-D1
    		Inhibitor
    ROCK-IN-D1 serves as a highly effective and selective inhibitor of ROCK.
    ROCK-IN-D1
  • HY-12798E
    (R)-AR-13503
    		Control 98.20%
    (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.
    (R)-AR-13503
  • HY-145294
    ROCK2-IN-5
    		Inhibitor
    ROCK2-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.
    ROCK2-IN-5
  • HY-156243
    GDI2-IN-1
    GDI2-IN-1 (compound (+)-37) is a GDP-dissociation inhibitor beta (GDI2) inhibitor with an IC50 of 2.87 μM and a KD of 36 μM. GDI2-IN-1 exhibits excellent in vivo antitumor activity in GDI2-overexpressing pancreatic xenograft models.
    GDI2-IN-1
  • HY-130011
    CCG-232964
    		Inhibitor
    CCG-232964 is an orally active inhibitor of Rho/MRTF/SRF. CCG-232964 inhibits LPA-induced CTGF gene expression.
    CCG-232964
  • HY-W047432
    5-Nitro-1H-indazole-3-carbonitrile
    		Inhibitor
    5-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.
    5-Nitro-1H-indazole-3-carbonitrile
  • HY-12880
    HA-100 dihydrochloride
    		Inhibitor
    HA-100 dihydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 dihydrochloride also used as a ROCK inhibitor.
    HA-100 dihydrochloride
  • HY-139061
    Palmitoyl 3-carbacyclic phosphatidic acid
    		Inhibitor
    Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model.
    Palmitoyl 3-carbacyclic phosphatidic acid
  • HY-118837
    WF-536
    		Inhibitor
    WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer.
    WF-536
  • HY-W295201
    ROCK-IN-11
    		Inhibitor
    ROCK-IN-11 (example 94) is a potent inhibitor of ROCK1 and ROCK2, with the IC50 of ≤ 5μM. ROCK-IN-11 plays an important role in cancer research.
    ROCK-IN-11
  • HY-176133
    ROCK-IN-12
    		Inhibitor
    ROCK-IN-12 (compound R3) is a selective ROCK inhibitor. ROCK-IN-12 can be used in the study of glaucoma.
    ROCK-IN-12
  • HY-153564
    ROCK-IN-6
    		Inhibitor
    ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. ROCK-IN-6 is extracted from patent WO2021164351 A1, example 7, has the potential for glaucoma and retinal diseases research.
    ROCK-IN-6
  • HY-175843
    ROCK2-IN-10
    		Inhibitor
    ROCK2-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.
    ROCK2-IN-10
  • HY-N12466
    3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine
    		Inhibitor
    3′-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.
    3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine
  • HY-116238
    ROCK-IN-D2
    		Inhibitor
    ROCK-IN-D2 is a potent and selective ROCK inhibitor.
    ROCK-IN-D2
  • HY-N15301
    Nocarnickelamide B
    		Inhibitor
    Nocarnickelamide 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.
    Nocarnickelamide B
  • HY-151189
    ROCK-IN-4
    		Inhibitor
    ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. ROCK-IN-4 reversibly depolymerizes F-actin, and suppresses mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 can be used for glaucoma or ocular hypertension research.
    ROCK-IN-4
  • HY-110335A
    OXA-06
    		Inhibitor
    OXA-06 is a pharmacologic inhibitor of ROCK, possessing antitumor activity by impairing cell migration and MYPT1 phosphorylation in PANC-1 cells.
    OXA-06
  • HY-15685A
    Ripasudil free base
    		Inhibitor
    Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
    Ripasudil free base
  • HY-103045A
    CMPD101 hydrochloride
    		Inhibitor
    CMPD101 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).
    CMPD101 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
ROCK Isoform Comparison

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