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Isoforms Recommended: ROCK1
Results for "

ROCK1

" in MedChemExpress (MCE) Product Catalog:

77

Inhibitors & Agonists

2

Peptides

3

Natural
Products

3

Recombinant Proteins

1

Isotope-Labeled Compounds

2

Antibodies

3

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10071
    Y-27632
    Maximum Cited Publications
    534 Publications Verification

    mTOR Ras ROCK NADPH Oxidase NF-κB Reactive Oxygen Species (ROS) Akt Apoptosis Autophagy PAK Cancer
    Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade [1] .
    Y-27632
  • HY-15307
    Belumosudil
    30+ Cited Publications

    KD025; SLx-2119

    ROCK Inflammation/Immunology Cancer
    Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties [1].
    Belumosudil
  • HY-15392
    Chroman 1
    60+ Cited Publications

    ROCK Cardiovascular Disease
    Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM [1] .
    Chroman 1
  • HY-10341
    Fasudil Hydrochloride
    25+ Cited Publications

    HA-1077 Hydrochloride; AT-877 Hydrochloride

    ROCK Calcium Channel Autophagy PKA PKC HIV Cancer
    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 Ca 2+ channel antagonist and vasodilator [1] .
    Fasudil Hydrochloride
  • HY-15556
    GSK269962A
    5+ Cited Publications

    GSK 269962

    ROCK Cardiovascular Disease Inflammation/Immunology
    GSK269962A (GSK 269962) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A has anti-inflammatory and vasodilatory activities [1].
    GSK269962A
  • HY-11000
    GSK429286A
    5+ Cited Publications

    ROCK Cancer
    GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
    GSK429286A
  • HY-10341A
    Fasudil
    25+ Cited Publications

    HA-1077; AT877

    ROCK Calcium Channel Autophagy PKA PKC Cancer
    Fasudil (HA-1077; AT877) 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 is also a potent Ca 2+ channel antagonist and vasodilator [1] .
    Fasudil
  • HY-15307A
    Belumosudil mesylate
    30+ Cited Publications

    KD025 mesylate; SLx-2119 mesylate

    ROCK Inflammation/Immunology
    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 [1].
    Belumosudil mesylate
  • HY-15685
    Ripasudil
    5+ Cited Publications

    K-115

    ROCK Cardiovascular Disease Neurological Disease
    Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
    Ripasudil
  • HY-15755
    RKI-1447
    4 Publications Verification

    ROCK Cancer
    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-10319
    BAY-549
    4 Publications Verification

    ROCK-IN-2; Azaindole 1; TC-S 7001

    ROCK Cardiovascular Disease
    BAY-549 (Azaindole 1), a chemical probe, 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 [1].
    BAY-549
  • HY-119937
    ROCK inhibitor-2
    2 Publications Verification

    ROCK Cardiovascular Disease Inflammation/Immunology Cancer
    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 [1] .
    ROCK inhibitor-2
  • HY-162596

    BA-1049 free base

    ROCK Neurological Disease
    NRL-1049 (BA-1049 (free base)) is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations [1] .
    NRL-1049
  • HY-108518

    ROCK Cardiovascular Disease Inflammation/Immunology
    SB-772077B dihydrochloride is an orally active aminofuran-based Rho kinase ((ROCK)) inhibitor with IC50 values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytokines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases [1] .
    SB-772077B dihydrochloride
  • HY-13911
    Hydroxyfasudil
    5 Publications Verification

    HA-1100

    ROCK Cardiovascular Disease Inflammation/Immunology Cancer
    Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
    Hydroxyfasudil
  • HY-15556A
    GSK269962A hydrochloride
    5+ Cited Publications

    GSK 269962 hydrochloride

    ROCK Cardiovascular Disease Inflammation/Immunology
    GSK269962A hydrochloride (GSK 269962 hydrochloride) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A hydrochloride has anti-inflammatory and vasodilatory activities [1].
    GSK269962A hydrochloride
  • HY-13911A
    Hydroxyfasudil hydrochloride
    5 Publications Verification

    HA-1100 hydrochloride; HA 1100 hydrochloride; HA1100 hydrochloride

    ROCK Cardiovascular Disease Inflammation/Immunology Cancer
    Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
    Hydroxyfasudil hydrochloride
  • HY-12437

    ROCK Cancer
    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-100270

    ROCK Cancer
    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 [1].
    Rho-Kinase-IN-1
  • HY-18990
    GSK180736A
    5+ Cited Publications

    ROCK G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    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-16758

    AR-12286

    ROCK Neurological Disease
    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 [1] .
    Verosudil
  • HY-10341C
    Fasudil dihydrochloride
    25+ Cited Publications

    HA-1077 dihydrochloride; AT-877 dihydrochloride

    Calcium Channel ROCK PKA PKC Autophagy HIV Cancer
    Fasudil (HA-1077; AT877) dihydrochloride 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 dihydrochloride is also a potent Ca 2+ channel antagonist and vasodilator [1] .
    Fasudil dihydrochloride
  • HY-Q22471
    ROCK1-IN-1
    1 Publications Verification

    ROCK Cardiovascular Disease
    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 [1].
    ROCK1-IN-1
  • HY-109191

    PHP-201; AMA0076

    ROCK Others
    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 [1] .
    Sovesudil
  • HY-100521
    GKI-1
    3 Publications Verification

    ROCK Cancer
    GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 μM against hGWL FL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 μM, but only weakly affected PKA [1].
    GKI-1
  • HY-15392A
    Chroman 1 dihydrochloride
    60+ Cited Publications

    ROCK Cardiovascular Disease
    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 [1] .
    Chroman 1 dihydrochloride
  • HY-149266
    THK01
    1 Publications Verification

    ROCK Cancer
    THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer [1].
    THK01
  • HY-125221

    ROCK Cdc42-binding kinase Cancer
    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 inhibits migration and invasion of cancer cells. DJ4 can be used for study of lung cancer, breast cancer, and pancreatic (PANC-1) cancer [1].
    DJ4
  • HY-109562A
    CCG258208 hydrochloride
    1 Publications Verification

    GRK2-IN-1 hydrochloride

    G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research [1].
    CCG258208 hydrochloride
  • HY-139690
    CCG258747
    1 Publications Verification

    Opioid Receptor G Protein-coupled Receptor Kinase (GRK) Mas-related G-protein-coupled Receptor (MRGPR) Cardiovascular Disease Inflammation/Immunology
    CCG258747 is a selective GRK2 inhibitor (IC50 = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance) [1] .
    CCG258747
  • HY-14362

    ROCK Ribosomal S6 Kinase (RSK) Cardiovascular Disease
    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) [1].
    GSK-25
  • HY-P10042

    Ribosomal S6 Kinase (RSK) Others
    S6K Substrate is a substrate for active protein kinases, including CLK2, MRCKalpha, MRCKbeta, p70S6K, ROCK1, ROCK2, RSK1, RSK3, PIM1 [1].
    S6K Substrate
  • HY-126432

    BA-1049

    ROCK Neurological Disease
    NRL-1049 dihydrochloride (BA-1049) is a selective and orally active rho-associated protein kinase 2 (ROCK2) inhibitor with an IC50 of 0.59 μM. NRL-1049 dihydrochloride shows selectivity for ROCK2 is 44 times that of ROCK1 (IC50 = 26 μM). NRL-1049 dihydrochloride can preserve the blood-brain barrier after acute injury [1].
    NRL-1049 dihydrochloride
  • HY-178821

    ROCK TGF-beta/Smad STAT Inflammation/Immunology
    ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0  nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research [1].
    ROCK2-IN-12
  • HY-N12378

    NF-κB Toll-like Receptor (TLR) PKA Epigenetic Reader Domain Keap1-Nrf2 Sirtuin AMPK Caspase FASTK ERK ROCK Apoptosis Metabolic Disease Inflammation/Immunology Cancer
    β-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. β-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. β-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. β-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma [1] .
    β-Patchoulene
  • HY-110339
    RKI-1447 dihydrochloride
    4 Publications Verification

    ROCK Apoptosis Cancer
    RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively [1]. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis .
    RKI-1447 dihydrochloride
  • HY-10071A
    Y-27632 hydrochloride hydrate
    395+ Cited Publications

    ROCK NF-κB Apoptosis Autophagy Akt mTOR NADPH Oxidase Reactive Oxygen Species (ROS) PAK Ras Neurological Disease Inflammation/Immunology Cancer
    Y-27632 hydrochloride hydrate is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 hydrochloride hydrate exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 hydrochloride hydrate enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 hydrochloride hydrate induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 hydrochloride hydrate promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade [1] .
    Y-27632 hydrochloride hydrate
  • HY-109562

    GRKs-IN-1

    G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research [1].
    CCG258208
  • HY-126257

    Akt Apoptosis Cancer
    AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells [1].
    AKT-IN-3
  • HY-RS12114

    Small Interfering RNA (siRNA) ROCK Others

    ROCK1 Human Pre-designed siRNA Set A contains three designed siRNAs for ROCK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    ROCK1 Human Pre-designed siRNA Set A
    ROCK1 Human Pre-designed siRNA Set A
  • HY-RS12116

    Small Interfering RNA (siRNA) Others

    Rock1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Rock1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Rock1 Rat Pre-designed siRNA Set A
    Rock1 Rat Pre-designed siRNA Set A
  • HY-RS12115

    Small Interfering RNA (siRNA) ROCK Others

    Rock1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Rock1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Rock1 Mouse Pre-designed siRNA Set A
    Rock1 Mouse Pre-designed siRNA Set A
  • HY-15685A

    K-115 free base

    ROCK Neurological Disease
    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-126275

    ROCK Cancer
    HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (Kds<2 nM). HSD1590 displays low cytotoxicity [1].
    HSD1590
  • HY-178013

    ROCK Inflammation/Immunology
    ROCK2-IN-11 (Compound A20) is a selective ROCK2 inhibitor with an IC50 of 0.18 μM for ROCK2 over ROCK1. ROCK2-IN-11 can be used for idiopathic pulmonary fibrosis and cGVHD research [1].
    ROCK2-IN-11
  • HY-109191A

    PHP-201 hydrochloride; AMA0076 hydrochloride

    ROCK Neurological Disease
    Sovesudil (PHP-201) hydrochloride 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 hydrochloride lowers intraocular pressure (IOP) without inducing hyperemia [1] .
    Sovesudil hydrochloride
  • HY-10833

    ROCK Cardiovascular Disease
    ROCK-IN-10 (compound 50) is a potent ROCK inhibitor with IC50 values of 6 nM and 4 nM for ROCK1 and ROCK2, respectively. ROCK-IN-10 shows >100-fold selectivity against other kinases [1].
    ROCK-IN-10
  • HY-118151

    ROCK Cardiovascular Disease Neurological Disease
    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 [1].
    Rho-Kinase-IN-3
  • HY-15685R

    K-115 (Standard)

    ROCK Reference Standards Cardiovascular Disease Neurological Disease
    Ripasudil (Standard) is the analytical standard of Ripasudil. This product is intended for research and analytical applications. Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
    Ripasudil (Standard)
  • HY-P10042A

    Ribosomal S6 Kinase (RSK) Others
    S6K Substrate acetate is a substrate for active protein kinases, including CLK2, MRCKalpha, MRCKbeta, p70S6K, ROCK1, ROCK2, RSK1, RSK3, PIM1 [1].
    S6K Substrate acetate

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