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 99.87%
    ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively.
    ROCK inhibitor-2
  • HY-18990
    GSK180736A
    Inhibitor 98.01%
    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-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-100984
    HA-100
    Inhibitor 99.80%
    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-15687A
    SAR407899
    Inhibitor 99.86%
    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-12659
    LX7101
    Inhibitor 99.75%
    LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.
    LX7101
  • HY-148808
    Zelasudil
    Inhibitor 99.86%
    Zelasudil is a Rho-associated (ROCK) kinase inhibitor. Zelasudil has a ROCK2 binding affinity.
    Zelasudil
  • HY-103045
    CMPD101
    Inhibitor 98.74%
    CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.
    CMPD101
  • HY-15727A
    Afuresertib hydrochloride
    Inhibitor 99.03%
    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
  • HY-13300
    SR-3677
    Inhibitor 99.90%
    SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
    SR-3677
  • HY-15687
    SAR407899 hydrochloride
    Inhibitor 98.66%
    SAR407899 hydrochloride 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 hydrochloride
  • HY-12437
    BDP5290
    Inhibitor 98.80%
    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-16758
    Verosudil
    Inhibitor 99.66%
    Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork.
    Verosudil
  • 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-13911
    Hydroxyfasudil
    Inhibitor 98.42%
    Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
    Hydroxyfasudil
  • 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-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-108518
    SB-772077B dihydrochloride
    Inhibitor ≥99.0%
    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-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-109191
    Sovesudil
    Inhibitor 98.31%
    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
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