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-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-125221
    DJ4
    Inhibitor 98.48%
    DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC50 values:5 and 50 nM) and MRCKα/β (IC50 values:10 and 100 nM). DJ4 blocks stress fiber formation and induces cell apoptosis. DJ4 can be used for study of cancer.
    DJ4
  • 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-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-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-122011
    PF-4950834
    Inhibitor
    PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration.
    PF-4950834
  • 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-10341D
    Fasudil mesylate
    Inhibitor
    Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active 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 mesylate is also a potent Ca2+ channel antagonist and vasodilator.
    Fasudil mesylate
  • HY-10341R
    Fasudil Hydrochloride (Standard)
    Inhibitor
    Fasudil (Hydrochloride) (Standard) is the analytical standard of Fasudil (Hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-19346
    AR-13324 analog mesylate
    ≥98.0%
    AR-13324 analog mesylate is an analog of AR-13324. AR-13324 is an ROCK and norepinephrine transporter (NET) inhibitor.
    AR-13324 analog mesylate
  • HY-121667
    Scaff10-8
    Inhibitor
    Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation.
    Scaff10-8
  • HY-12659B
    LX7101 monohydrochloride
    Inhibitor
    LX7101 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.
    LX7101 monohydrochloride
  • HY-116420
    ROCK2-IN-8
    Inhibitor
    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-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
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