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

ROCK

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

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12659
    LX7101
    Inhibitor 99.54%
    LX7101 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 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 has the potential for ocular hypertension and associated glaucoma research.
    LX7101
  • HY-Y0078
    Cinnamyl Alcohol
    Inhibitor 99.80%
    Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, exhibits anti-obesity, antioxidant and anti-inflammatory activities.
    Cinnamyl Alcohol
  • HY-18713
    CRT0066854
    Inhibitor 99.54%
    CRT0066854 is a potent and selective atypical PKC isoenzymes inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively.
    CRT0066854
  • HY-12437
    BDP5290
    Inhibitor 98.90%
    BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
    BDP5290
  • HY-13911A
    Hydroxyfasudil hydrochloride
    Inhibitor 98.88%
    Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
    Hydroxyfasudil hydrochloride
  • HY-100521
    GKI-1
    Inhibitor 99.96%
    GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 μM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 μM, but only weakly affected PKA.
    GKI-1
  • HY-16663
    ITX3
    Inhibitor 98.60%
    ITX3 is a specific and nontoxic inhibitor of TrioN (N-terminal GEF domain of the multidomain Trio protein) with an IC50 value of 76 μM. ITX3 can be used for the research of agent.
    ITX3
  • HY-13911
    Hydroxyfasudil
    Inhibitor 98.78%
    Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
    Hydroxyfasudil
  • HY-150640
    Rho-Kinase-IN-2
    Inhibitor 98.80%
    Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research.
    Rho-Kinase-IN-2
  • HY-16758
    Verosudil
    Inhibitor 99.18%
    Verosudil (AR-12286) is a ROCK inhibitor. Verosudil has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil increases trabecular outflow capacity to reduce intraocular pressure. Verosudil is useful in the study of glaucoma and ocular hypertension.
    Verosudil
  • HY-167832
    PT109
    Inhibitor 99.20%
    PT109 is a multi-kinase inhibitor. PT109 inhibits JNK (JNK1: IC50=0.143 μM; JNK2: IC50=0.831 μM; JNK3: IC50=0.285 μM) and other kinases (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM; ROCK2: IC50=34 μM) and plays an important role in anti-inflammation, anti-oxidation, neurogenesis, synaptogenesis, etc. In addition, PT109 also reprograms glioblastoma multiforme (GBM) into oligodendrocytes through the PTBP1/PKM1/2 pathway and changes the metabolic pattern of GBM, exerting anti-glioma activity.
    PT109
  • HY-100270
    Rho-Kinase-IN-1
    Inhibitor 99.91%
    Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008.
    Rho-Kinase-IN-1
  • HY-109191
    Sovesudil
    Inhibitor 99.91%
    Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil lowers intraocular pressure (IOP) without inducing hyperemia.
    Sovesudil
  • HY-15392A
    Chroman 1 dihydrochloride
    Inhibitor 99.11%
    Chroman 1 dihydrochloride is a highly potent and selective ROCK inhibitor. Chroman 1 dihydrochloride is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 dihydrochloride also has inhibitory activity against MRCK, with an IC50 of 150 nM.
    Chroman 1 dihydrochloride
  • HY-Q22471
    ROCK1-IN-1
    Inhibitor 98.86%
    ROCK1-IN-1 is a ROCK1 inhibitor with a Ki value of 540 nM. ROCK1-IN-1 can be used for the research of hypertension, glaucoma and erectile dysfunction.
    ROCK1-IN-1
  • HY-125639
    (rac)-AR-13503
    Inhibitor 99.08%
    (rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice.
    (rac)-AR-13503
  • HY-14362
    GSK-25
    Inhibitor 99.68%
    GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).
    GSK-25
  • HY-18713A
    CRT0066854 hydrochloride
    Inhibitor 99.29%
    CRT0066854 hydrochloride is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively.
    CRT0066854 hydrochloride
  • HY-116420
    ROCK2-IN-8
    Inhibitor 99.85%
    ROCK2-IN-8 (Compound 1) is an orally active ROCK2 inhibitor, with an IC50 of 7.2 nM. ROCK2-IN-8 can be used for the research of aqueous humor outflow in porcine eyes and myosin light chain phosphorylation.
    ROCK2-IN-8
  • HY-132302
    Hu7691
    Inhibitor 99.91%
    Hu7691 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 inhibits tumor growth and enables decrease of cutaneous toxicity in mice.
    Hu7691
Cat. No. Product Name / Synonyms Application Reactivity

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