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-10341C
    Fasudil dihydrochloride
    		Inhibitor 99.98%
    Fasudil (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.
    Fasudil dihydrochloride
  • HY-100035
    PT-262
    		Inhibitor 99.21%
    PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity.
    PT-262
  • HY-P2325
    Exoenzyme C3, clostridium botulinum
    		Inhibitor
    Exoenzyme C3, clostridium botulinum, is a mono-ADP-ribosylating enzyme. Exoenzyme C3, clostridium botulinum specifically modifies RhoA, B, and C by transferring ADP-ribose to them, thereby inactivating these GTPases. Exoenzyme C3, clostridium botulinum can induce neuronal axonal and dendritic growth, inhibit macrophage migration, and regulate cytoskeletal dynamics. Exoenzyme C3, clostridium botulinum can be used in the research of spinal cord injury and diabetic painful neuropathy.
    Exoenzyme C3, clostridium botulinum
  • HY-162596
    NRL-1049
    		Inhibitor 99.87%
    NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59 µM and 26 µM for ROCK2 and ROCK1 respectively). NRL-1049 reduces Lysophosphatidic acid induced ROCK activation in endothelial cells. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice.
    NRL-1049
  • HY-15720B
    Glycyl H-1152 hydrochloride
    		Inhibitor 99.9%
    Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC50s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride.
    Glycyl H-1152 hydrochloride
  • HY-126913
    Rhodblock 6
    		Inhibitor 98.94%
    Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization.
    Rhodblock 6
  • HY-107209
    RKI-1313
    		Inhibitor 98.2%
    RKI-1313 is a ROCK inhibitor with IC50s of 34, 8 µM for ROCK 1 and ROCK 2, respectively. RKI-1313 shows little effect on the phosphorylation levels of ROCK substrates, migration, invasion or anchorage-independent growth.
    RKI-1313
  • HY-RS12119
    Rock2 Rat Pre-designed siRNA Set A
    		Inhibitor

    Rock2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Rock2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Rock2 Rat Pre-designed siRNA Set A
  • HY-10071A
    Y-27632 hydrochloride hydrate
    		Inhibitor
    Y-27632 hydrochloride hydrate is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 hydrochloride hydrate attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 hydrochloride hydrate also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 hydrochloride hydrate primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
    Y-27632 hydrochloride hydrate
  • HY-132302A
    Hu7691 free base
    		Inhibitor
    Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
    Hu7691 free base
  • HY-172177
    ROCK/HDAC-IN-2
    		Inhibitor
    ROCK/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).
    ROCK/HDAC-IN-2
  • HY-10341B
    Fasudil hydrochloride semihydrate
    		Inhibitor
    Fasudil (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.
    Fasudil hydrochloride semihydrate
  • HY-RS12118
    Rock2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Rock2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Rock2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Rock2 Mouse Pre-designed siRNA Set A
  • HY-153011
    ROCK-IN-5
    		Inhibitor ≥98.0%
    ROCK-IN-5 (compound I-B-37) is a potent inhibitor of ROCK, ERK, GSK, and AGC protein kinases. ROCK-IN-5 has the potential for proliferative, cardiac and neurodegenerative diseases research.
    ROCK-IN-5
  • HY-134913
    Rhodblock 1a
    		Inhibitor
    Rhodblock 1a is an inhibitor of the Rho kinase signaling pathway. It inhibits the normal formation of the cleavage furrow during cell division by interfering with the localization and function of Rho pathway proteins, causing some cells to fail to form a cleavage furrow or the formed cleavage furrow to break, resulting in binucleated cells. Rhodblock 1a can be used to study the mechanism of cell division and is expected to be used in the research of diseases such as cardiovascular diseases and cancer.
    Rhodblock 1a
  • HY-168650
    ROCK/HDAC-IN-1
    		Inhibitor
    ROCK/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.
    ROCK/HDAC-IN-1
  • HY-16563R
    Narciclasine (Standard)
    		Activator
    Narciclasine (Standard) is the analytical standard of Narciclasine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-16758A
    Verosudil hydrochloride
    		Inhibitor
    Verosudil (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.
    Verosudil hydrochloride
  • HY-100460
    BIPM
    		Inhibitor
    BIPM is a potent ROCK2 inhibitor. BIPM leads to significant changes in neurite length, cell migration and actin stress fibers. BIPM plays an important role in anti-cancer metastasis.
    BIPM
  • HY-162798
    ROCK2-IN-9
    		Inhibitor
    ROCK2-IN-9 (compound 7u) is a selective ROCK2 inhibitor (IC50=36.8 nM) with anticancer activity. ROCK2-IN-9 inhibits cancer cell migration and invasion by regulating multiple cellular activities of the actin cytoskeleton. ROCK2-IN-9 can be used in breast cancer research.
    ROCK2-IN-9
Cat. No. Product Name / Synonyms Application Reactivity
ROCK Isoform Comparison

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