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-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-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-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-118151
    Rho-Kinase-IN-3
    		Inhibitor
    Rho-Kinase-IN-3 (compound 12) is a potent and selective Rho kinase (ROCK1) inhibitor with an IC50 value of 8 nM. Rho-Kinase-IN-3 can be used in research of hypertension.
    Rho-Kinase-IN-3
  • 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-130448
    8-iso Prostaglandin F1β
    		Activator
    8-iso Prostaglandin F1β is an isoprostane, that exhibits vasoconstrictive effect in neonatal porcine pulmonary arteries, pulmonary veins, and mesenteric arteries. 8-iso Prostaglandin F1β targets TXA2 receptor and exhibits the blood vessel contractile efficacy under the influence of tyrosine kinase and Rho kinase.
    8-iso Prostaglandin F1β
  • 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-15307S
    Belumosudil-d7
    		Inhibitor
    Belumosudil-d7 (KD025-d7) is deuterium labeled Belumosudil. 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-d<sub>7</sub>
  • 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-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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