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-119937
    ROCK inhibitor-2
    Inhibitor 99.92%
    ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC50 of 75 nM. ROCK inhibitor-2 exhibits antitumor activity.
    ROCK inhibitor-2
  • HY-16071
    AT13148
    Inhibitor 99.20%
    AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
    AT13148
  • HY-12798B
    Netarsudil hydrochloride
    Inhibitor 99.90%
    Netarsudil (AR-13324) hydrochloride is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil hydrochloride 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 hydrochloride is mainly used in the study of ocular hypertension and primary open-angle glaucoma.
    Netarsudil hydrochloride
  • HY-15755
    RKI-1447
    Inhibitor 98.29%
    RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
    RKI-1447
  • HY-15307A
    Belumosudil mesylate
    Inhibitor 99.89%
    Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
    Belumosudil mesylate
  • HY-10069
    Y-33075 dihydrochloride
    Inhibitor 98.02%
    Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
    Y-33075 dihydrochloride
  • HY-121750
    CCG-222740
    Inhibitor 99.53%
    CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
    CCG-222740
  • HY-13300
    SR-3677
    Inhibitor 99.83%
    SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
    SR-3677
  • HY-15720
    H-1152
    Inhibitor 98.63%
    H-1152 is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
    H-1152
  • HY-15687A
    SAR407899
    Inhibitor 99.60%
    SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation.
    SAR407899
  • HY-12798C
    AR-13503
    Inhibitor 98.21%
    AR-13503 (AR-13324 M1 metabolite) is the hydrolytic metabolite of AR-13324 mesylate. AR-13324 is a ROCK kinase and PKC inhibitor with anti-angiogenic and retinal health-improving effects, showing potential for use in retinal disease research.
    AR-13503
  • 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-100984
    HA-100
    Inhibitor 99.87%
    HA-100 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 also used as a ROCK inhibitor.
    HA-100
  • HY-10319
    BAY-549
    Inhibitor 99.46%
    BAY-549 (Azaindole 1) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively.
    BAY-549
  • HY-12798A
    Netarsudil dimesylate
    99.90%
    Netarsudil (AR-13324) dimesylate is a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). Netarsudil dimesylate 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 dimesylate is mainly used in the study of ocular hypertension and primary open-angle glaucoma.
    Netarsudil dimesylate
  • 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-108518
    SB-772077B dihydrochloride
    Inhibitor 99.33%
    SB-772077B dihydrochloride is an aminofurazan-based Rho kinase (ROCK) inhibitor with IC50s of 5.6 nM and 6 nM toward ROCK1 and ROCK2, respevtively.
    SB-772077B dihydrochloride
  • HY-18990
    GSK180736A
    Inhibitor 98.81%
    GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
    GSK180736A
  • 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-15727A
    Afuresertib hydrochloride
    Inhibitor 99.95%
    Afuresertib hydrochloride (GSK 2110183 hydrochloride) 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 hydrochloride
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