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ROCK2 inhibitor

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78

Inhibitors & Agonists

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Isotope-Labeled Compounds

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

    ROCK NADPH Oxidase mTOR Reactive Oxygen Species (ROS) NF-κB Apoptosis Akt Autophagy PAK Ras 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 .
    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 .
    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 .
    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 .
    Fasudil Hydrochloride
  • HY-103045
    CMPD101
    4 Publications Verification

    ROCK PKC G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    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-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 .
    GSK269962A
  • 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 .
    Fasudil
  • HY-148808

    RXC007

    ROCK Cancer
    Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma .
    Zelasudil
  • 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 .
    Belumosudil mesylate
  • HY-15720A
    H-1152 dihydrochloride
    4 Publications Verification

    ROCK Neurological Disease
    H-1152 dihydrochloride 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 dihydrochloride
  • 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 .
    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 .
    ROCK inhibitor-2
  • HY-15687A
    SAR407899
    3 Publications Verification

    ROCK Metabolic Disease
    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-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 .
    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 .
    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-15720
    H-1152
    4 Publications Verification

    ROCK Neurological Disease
    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-103620

    ROCK Inflammation/Immunology Cancer
    ROCK2-IN-2 (Example 2) is a ROCK2 inhibitor that can be used for the study of multiple medical disorders, such as fibrosis, inflammatory disorders, autoimmune disorders, and cardiovascular disorders .
    ROCK2-IN-2
  • 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-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 .
    GSK269962A hydrochloride
  • 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 .
    Rho-Kinase-IN-1
  • 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 .
    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 .
    Fasudil dihydrochloride
  • HY-12659
    LX7101
    3 Publications Verification

    LIM Kinase (LIMK) ROCK PKA Endocrinology
    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-15687
    SAR407899 hydrochloride
    3 Publications Verification

    ROCK Metabolic Disease
    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-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 .
    THK01
  • HY-150640

    ROCK Neurological Disease Inflammation/Immunology Cancer
    Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and CNS-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50 = 3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research .
    Rho-Kinase-IN-2
  • 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 .
    Chroman 1 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 .
    ROCK2-IN-12
  • HY-156592A

    ROCK Inflammation/Immunology
    ROCK2-IN-6 hydrochloride (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research .
    ROCK2-IN-6 hydrochloride
  • 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 .
    NRL-1049 dihydrochloride
  • HY-116420

    ROCK Neurological Disease
    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-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 . RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis .
    RKI-1447 dihydrochloride
  • 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 .
    ROCK2-IN-11
  • 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 .
    Y-27632 hydrochloride hydrate
  • 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 .
    HSD1590
  • HY-175843

    ROCK STAT Cancer
    ROCK2-IN-10 is a potent and selective ROCK2 inhibitor (IC50 = 0.020 μM) with 41-fold selectivity over isoform ROCK1. ROCK2-IN-10 inhibits metastasis by disrupting the cytoskeleton, independent of proliferative suppression. ROCK2-IN-10 shows superior inhibitory potency against cancer cell metastasis, which closely related to the suppression of STAT3 phosphorylation. ROCK2-IN-10 can be used for breast cancer metastasis research .
    ROCK2-IN-10
  • HY-15307AR

    KD025 mesylate (Standard); SLx-2119 mesylate (Standard)

    ROCK Reference Standards Inflammation/Immunology Cancer
    Belumosudil (mesylate) (Standard) is the analytical standard of Belumosudil (mesylate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-15307R

    KD025 (Standard); SLx-2119 (Standard)

    ROCK Reference Standards Inflammation/Immunology Cancer
    Belumosudil (Standard) is the analytical standard of Belumosudil. This product is intended for research and analytical applications. 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 (Standard)
  • HY-U00351
    ROCK-IN-1
    1 Publications Verification

    ROCK Cardiovascular Disease Inflammation/Immunology
    ROCK-IN-1 is a potent inhibitor of ROCK, with an IC50 of 1.2 nM for ROCK2.
    ROCK-IN-1
  • HY-149700

    ROCK MMP STAT Others
    ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model .
    ROCK2-IN-7
  • HY-162798

    ROCK Cancer
    ROCK2-IN-9 (compound 7u) is a selective ROCK2 inhibitor (IC50=36.8 nM) with anticancer activity. ROCK2-IN-9 inhibits cancer cell migration and invasion by regulating multiple cellular activities of the actin cytoskeleton. ROCK2-IN-9 can be used in breast cancer research .
    ROCK2-IN-9
  • 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-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 .
    ROCK-IN-10
  • HY-122011

    ROCK SGK PKA PKC Inflammation/Immunology
    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-103045A

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