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

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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-10071
    Y-27632
    		Inhibitor 99.91%
    Y-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.
    Y-27632
  • HY-10583
    Y-27632 dihydrochloride
    		Inhibitor 99.98%
    Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects.
    Y-27632 dihydrochloride
  • HY-15392
    Chroman 1
    		Inhibitor 98.97%
    Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM.
    Chroman 1
  • HY-10341
    Fasudil Hydrochloride
    		Inhibitor 99.97%
    Fasudil (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.
    Fasudil Hydrochloride
  • HY-13257
    Thiazovivin
    		Inhibitor 99.97%
    Thiazovivin is a potent ROCK inhibitor, which can protect human embryonic stem cells. Thiazovivin improves the efficiency of iPSC generation.
    Thiazovivin
  • HY-126432
    NRL-1049 dihydrochloride
    		Inhibitor 99.20%
    NRL-1049 dihydrochloride (BA-1049) is a selective and orally active rho-associated protein kinase 2 (ROCK2) inhibitor with an IC50 of 0.59 μM. NRL-1049 dihydrochloride shows selectivity for ROCK2 is 44 times that of ROCK1 (IC50 = 26 μM). NRL-1049 dihydrochloride can preserve the blood-brain barrier after acute injury.
    NRL-1049 dihydrochloride
  • HY-181582
    LASSBio-2382
    		Inhibitor
    LASSBio-2382 is a dual ROCK1/ROCK2 inhibitor with ROCK1 IC50 of 0.005 μM and ROCK2 IC50 of 0.003 μM. LASSBio-2382 inhibits viability and migration of cancer cells. LASSBio-2382 can be used for the research of triple-negative breast cancer.
    LASSBio-2382
  • HY-179498
    ROCK2-IN-13
    		Inhibitor
    ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G2/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach.
    ROCK2-IN-13
  • HY-15307
    Belumosudil
    		Inhibitor 99.83%
    Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
    Belumosudil
  • HY-10583R
    Y-27632 dihydrochloride (Standard)
    		Inhibitor
    Y-27632 dihydrochloride (Standard) is the analytical standard of Y-27632 dihydrochloride. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects.
    Y-27632 dihydrochloride (Standard)
  • HY-10583G
    Y-27632 dihydrochloride (GMP)
    		Inhibitor
    Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect.
    Y-27632 dihydrochloride (GMP)
  • HY-16563
    Narciclasine
    		Activator 99.88%
    Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
    Narciclasine
  • HY-103045
    CMPD101
    		Inhibitor 98.96%
    CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
    CMPD101
  • HY-15727
    Afuresertib
    		Inhibitor 99.53%
    Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.
    Afuresertib
  • HY-15556
    GSK269962A
    		Inhibitor 99.75%
    GSK269962A (GSK 269962) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A has anti-inflammatory and vasodilatory activities.
    GSK269962A
  • HY-11000
    GSK429286A
    		Inhibitor 98.27%
    GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
    GSK429286A
  • HY-12798
    Netarsudil
    		Inhibitor 99.94%
    Netarsudil (AR-13324) is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil reduces intraocular pressure by inhibiting ROCK, causing relaxation of trabecular meshwork cells and dilation of episcleral veins, thereby increasing the ease of aqueous humor outflow, while inhibiting NET to reduce aqueous humor production. Netarsudil is mainly used in the study of ocular hypertension and primary open-angle glaucoma.
    Netarsudil
  • HY-148808
    Zelasudil
    		Inhibitor 99.48%
    Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma.
    Zelasudil
  • HY-15685
    Ripasudil
    		Inhibitor 99.95%
    Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
    Ripasudil
  • HY-10341A
    Fasudil
    		Inhibitor 99.98%
    Fasudil (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.
    Fasudil
Cat. No. Product Name / Synonyms Application Reactivity
ROCK Isoform Comparison

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