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Rho Inhibitors

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-12649
    Y16
    5 Publications Verification

    Ras Cancer
    Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP .
    Y16
  • 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-126913

    ROCK Cancer
    Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization .
    Rhodblock 6
  • HY-172917

    Ras Cancer
    Rho GTPase inhibitor 1 (compound 7) is a potent Rho GTPase inhibitor. Rho GTPase inhibitor 1 exhibits high affinity on Cdc42, Rac1 and RhoA with KDs of 151, 352, and 232 μM, respectively. Rho GTPase inhibitor 1 reduces cell migration on glioma cell line .
    Rho GTPase inhibitor 1
  • 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 .
    Rho-Kinase-IN-3
  • HY-158652

    Ras Akt PI3K Cancer
    (R)-CCG-1423 is an inhibitor of RhoA. (R)-CCG-1423 inhibits downstream of Rho and shows specificity for SRE .
    (R)-CCG-1423
  • HY-130011

    ROCK Ras Neurological Disease Cancer
    CCG-232964 is an orally active inhibitor of Rho/MRTF/SRF. CCG-232964 inhibits LPA-induced CTGF gene expression .
    CCG-232964
  • HY-P5158

    Adrenergic Receptor Others
    Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
    Conopeptide rho-TIA
  • HY-134913

    ROCK Cardiovascular Disease Cancer
    Rhodblock 1a is an inhibitor of the Rho kinase signaling pathway. It inhibits the normal formation of the cleavage furrow during cell division by interfering with the localization and function of Rho pathway proteins, causing some cells to fail to form a cleavage furrow or the formed cleavage furrow to break, resulting in binucleated cells. Rhodblock 1a can be used to study the mechanism of cell division and is expected to be used in the research of diseases such as cardiovascular diseases and cancer .
    Rhodblock 1a
  • 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-117149

    Ras Cancer
    MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases .
    MLS000532223
  • HY-17543
    ML-323
    10+ Cited Publications

    Deubiquitinase Cancer
    ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
    ML-323
  • 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-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-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-120429

    Apoptosis Cancer
    SKLB-163 is an orally active inhibitor for Rho GDP-dissociation (RhoGDI). SKLB-163 inhibits highly expressed RhoGDI tumor cell proliferation and migration, and increases radiosensitivity of tumor cells. SKLB-163 induces cancer cell Apoptosis .
    SKLB-163
  • 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-111432

    Ras Others
    CCG-232601 (compound 8f) is a potent and orally active Rho/MRTF/SRF transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma .
    CCG-232601
  • HY-10583
    Y-27632 dihydrochloride
    Maximum Cited Publications
    330 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-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-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-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-13991
    CCG-1423
    10+ Cited Publications

    Ras Apoptosis Cancer
    CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
    CCG-1423
  • HY-121750

    Ras ROCK Cancer
    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-111458
    GSK2643943A
    5 Publications Verification

    Deubiquitinase Cancer
    GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
    GSK2643943A
  • HY-I0400
    N-Acetylneuraminic acid
    3 Publications Verification

    NANA; Lactaminic acid

    Tyrosinase Ras Influenza Virus Endogenous Metabolite Cardiovascular Disease Inflammation/Immunology Cancer
    N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia .
    N-Acetylneuraminic acid
  • HY-108361
    CCG-203971
    1 Publications Verification

    Ras Inflammation/Immunology Cancer
    CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent .
    CCG-203971
  • 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
  • HY-10583R
    Y-27632 (dihydrochloride) (Standard)
    Maximum Cited Publications
    330 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-I0400R

    Tyrosinase Ras Influenza Virus Endogenous Metabolite Cardiovascular Disease Inflammation/Immunology Cancer
    N-Acetylneuraminic acid (Standard) is the analytical standard of N-Acetylneuraminic acid. This product is intended for research and analytical applications. N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia .
    N-Acetylneuraminic acid (Standard)
  • HY-105284R

    Beta-lactamase Bacterial Antibiotic Infection
    N-Acetylneuraminic acid (Standard) is the analytical standard of N-Acetylneuraminic acid. This product is intended for research and analytical applications. N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia .
    Sulopenem (Standard)
  • HY-12646A

    Ras Apoptosis Cancer
    Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis . Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
    Rhosin
  • 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-12646
    Rhosin hydrochloride
    25+ Cited Publications

    Ras Apoptosis Cancer
    Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis . Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability .
    Rhosin hydrochloride
  • HY-173222

    P-glycoprotein Cancer
    P-gp inhibitor 28 (Compound 4h) is an inhibitor targeting P-glycoprotein (P-gp). It can inhibit the proliferation of cancer cells, and its IC50 value for MCF-7/ADR cells is between 15.88 and 21.96 μM. P-gp inhibitor 28 can increase the accumulation of Rho123 in MCF-7/ADR cells and can be used in research related to cancer and overcoming multidrug resistance in tumors .
    P-gp inhibitor 28
  • HY-134817
    USP7-IN-8
    1 Publications Verification

    Deubiquitinase Cancer
    USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects .
    USP7-IN-8
  • HY-118046

    ROCK IGF-1R G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that can be used as a probe for studying heart failure and Parkinson's disease. GSK2163632A potently inhibits GRK1 and GRK5, and also inhibits Rho-associated coiled-coil kinase (ROCK) and insulin-like growth factor receptor IGF-1R. GSK2163632A binds to GRK2 in a manner similar to Paroxetine (HY-122272).
    GSK2163632A
  • HY-12798

    AR-13324

    Monoamine Transporter ROCK Cardiovascular Disease Neurological Disease
    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-12798B

    AR-13324 hydrochloride

    ROCK Cardiovascular Disease Neurological Disease
    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-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-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-12798A

    AR-13324 dimesylate

    ROCK Cardiovascular Disease Neurological Disease
    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-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-B0515B

    Apoptosis Metabolic Disease Cancer
    Ibandronate Sodium is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium inhibits tumor cell proliferation (such as ER+ breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
    Ibandronate Sodium
  • HY-13991A

    Ras Metabolic Disease Cancer
    (S)-CCG-1423 is an inhibitor of Rho signaling that blocks the nuclear import of MRTF-A. (S)-CCG-1423 reduces the nuclear accumulation of MRTF-A and improves glucose uptake and tolerance in insulin-resistance mice in vivo. (S)-CCG-1423 exhibits higher inhibition activity than the SR- and the R-isomers of CCG-1423 (HY-13991). (S)-CCG-1423 can be used for the research of cancer and diabetes .
    (S)-CCG-1423
  • 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-12755
    ML141
    25+ Cited Publications

    CID-2950007

    Ras Apoptosis Cancer
    ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
    ML141
  • HY-152095

    Ras Cancer
    PPI-GIT1/β-Pix interaction-IN-1 is a potent and orally active GIT1/β-Pix protein-protein interaction (PPI) inhibitor with a KD value of 7.7 µM. PPI-GIT1/β-Pix interaction-IN-1 disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42. PPI-GIT1/β-Pix interaction-IN-1 inhibits metastasis of gastric cancer .
    PPI-GIT1/β-Pix interaction-IN-1
  • HY-B0515

    BM-210955; RPR-102289A

    Apoptosis Metabolic Disease Cancer
    Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium Monohydrate can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium Monohydrate inhibits tumor cell proliferation (such as ER + breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium Monohydrate is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
    Ibandronate Sodium Monohydrate

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