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Rho kinase

" in MedChemExpress (MCE) Product Catalog:

32

Inhibitors & Agonists

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-150640

    ROCK Neurological Disease
    Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (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-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-112362

    Rockout; 3-(4-Pyridinyl)-1H-indole; Rho kinase Inhibitor III, Rockout

    ROCK Inflammation/Immunology
    3-(4-Pyridyl)indole (Rockout) is a Rho-kinase (ROCK) inhibitor, with an IC50 of 25 μM. 3-(4-Pyridyl)indole can inhibit blebbing and cause dissolution of actin stress fibers in a wound healing assay .
    3-(4-Pyridyl)indole
  • HY-126913

    ROCK Cancer
    Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization .
    Rhodblock 6
  • HY-139170

    ROCK Metabolic Disease
    CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR) .
    CAY10746
  • HY-16563
    Narciclasine
    10+ Cited Publications

    Lycoricidinol

    ROCK Cancer
    Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
    Narciclasine
  • HY-12798A

    AR-13324 dimesylate

    ROCK Others
    Netarsudil mesylate (AR-13324 mesylate) is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.
    Netarsudil dimesylate
  • HY-118151

    ROCK 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 .
    Rho-Kinase-IN-3
  • HY-145294

    ROCK Neurological Disease
    ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation .
    ROCK2-IN-5
  • HY-16563R

    ROCK Cancer
    Narciclasine (Standard) is the analytical standard of Narciclasine. This product is intended for research and analytical applications. Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.
    Narciclasine (Standard)
  • HY-12798

    AR-13324

    Monoamine Transporter ROCK Neurological Disease
    Netarsudil is a Rho kinase (ROCK) and norepinephrine transporter (NET) inhibitor. Netarsudil increases outflow facility in human eyes through multiple mechanisms .
    Netarsudil
  • HY-108518

    ROCK Cardiovascular Disease
    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
    5 Publications Verification

    ROCK 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-N6012

    Apoptosis Inflammation/Immunology Cancer
    (-)-Alkannin, found in Alkanna tinctoria, is used as a food coloring. (-)-Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. (-)-Alkannin improves hepatic inflammation in a Rho-kinase pathway .
    (-)-Alkannin
  • 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-118837

    ROCK Cancer
    WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer .
    WF-536
  • HY-10583
    Y-27632 dihydrochloride
    Maximum Cited Publications
    273 Publications Verification

    Organoid ROCK Neurological Disease Cancer
    Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects .
    Y-27632 dihydrochloride
  • 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 .
    Sovesudil
  • 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 .
    Sovesudil hydrochloride
  • HY-15392
    Chroman 1
    20+ 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-15392A
    Chroman 1 dihydrochloride
    20+ 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-16758

    AR-12286

    ROCK Neurological Disease
    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-16758A

    AR-12286 hydrochloride

    ROCK Others
    Verosudil hydrochloride (AR-12286 hydrochloride) is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is an inhibitor for Rho-kinase (ROCK) with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. Verosudil hydrochloride lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork .
    Verosudil hydrochloride
  • HY-10583R
    Y-27632 dihydrochloride (Standard)
    Maximum Cited Publications
    273 Publications Verification

    ROCK Organoid Cancer
    Y-27632 (dihydrochloride) (Standard) is the analytical standard of Y-27632 (dihydrochloride). Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects .
    Y-27632 dihydrochloride (Standard)
  • HY-103045A

    PKC ROCK 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
  • HY-15720B

    ROCK Aurora Kinase CaMK Neurological Disease
    Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC50s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride .
    Glycyl H-1152 hydrochloride
  • HY-10583G

    ROCK Neurological Disease Cancer
    Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect .
    Y-27632 dihydrochloride
  • HY-137638

    PKA Metabolic Disease
    Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U46619-induced activation of Rho, Gq and G12/G13 in platelets .
    Sp-5,6-DCl-cBIMPS
  • HY-137638A

    Sp-5,6-DCI-cBIMPS

    PKA Metabolic Disease
    Sp-5,6-DCl-cBIMPS sodium is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS sodium stimulates insulin release. Sp-5,6-DCl-cBIMPS sodium inhibits U-46619 (HY-108566)-induced activation of Rho, Gq and G12/G13 in platelets .
    Sp-5,6-DCl-cBIMPS sodium
  • 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-P10636

    LRRK2 Others
    Nictide is a peptide substrate of LRRK2 (leucine-rich repeat protein kinase-2). Nictide can be phosphorylated by the activated LRRK2[G2019S] with a Km of 10 μM .
    Nictide
  • HY-118046

    G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that may serve as a probe for studying heart failure and Parkinson's disease. Screening of known protein kinase inhibitors by differential scanning fluorescence method revealed that the melting points of GRK2 and GRK5 increased. Enzymatic assays of the 14 most stable hits revealed that three exhibited nanomolar inhibitory potency against a single GRK, with some showing significant selectivity. Most of the identified compounds can be divided into two categories: indazole/dihydropyrimidine compounds selectively inhibit GRK2, and pyrrolopyrimidine compounds effectively inhibit GRK1 and GRK5 but with modest selectivity. The two most inhibitory representative compounds, GSK180736A and GSK2163632A, are co-crystals with GRK2 and GRK1, respectively, and their atomic structures were determined to 2.6 and 1.85 ? distances, respectively. GSK180736A, as an inhibitor of Rho-related coiled-coil protein kinase, binds to GRK2 in a manner similar to paroxetine, while GSK2163632A, as an inhibitor of insulin-like growth factor 1 receptor, occupies a novel region of the GRK active site cleft and may be used to achieve more Selectivity. However, both compounds inhibited GRK no more potently than their original targets. These data provide a basis for the rational design of more effective and selective GRK inhibitors in the future .
    GSK2163632A

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