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ROCK

Rho-associated protein kinase (ROCK) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. It is involved mainly in regulating the shape and movement of cells by acting on the cytoskeleton.

  • Y-27632 dihydrochloride
    T1725129830-38-2
    Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.
    • $39
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  • Y-27632
    T1870146986-50-7
    Y-27632 is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.
    • $39
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  • Chroman 1
    T149601273579-40-0In house
    Chroman 1 is an inhibitor of ROCK2 (IC50: 1 nM).
    • $70
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  • Zelasudil
    T696652365193-22-0
    Zelasudil (RXC007) is a Rho-related (ROCK) kinase inhibitor for the study of idiopathic pulmonary fibrosis and inflammation.
    • $322
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  • Ripasudil
    TQ0319887375-67-9
    Ripasudil (Ripasudil hydrochloride dihydrate) (K-115) hydrochloride dihydrate is a specific ROCK inhibitor (IC50s: 51 19 nM for ROCK1 ROCK2).
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    • Netarsudil Dihydrochloride
      T103581253952-02-1
      Netarsudil Dihydrochloride (AR-13324 Dihydrochloride) is an inhibitor of Rho-associated protein kinase (ROCK) and norepinephrine transporter (NET) with effective in intraocular pressure (IOP) reduction.
      • $50
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    • Narciclasine
      TQ018329477-83-6
      Narciclasine (Lycoricidinol), a natural product, modulates the Rho Rho-kinase LIM kinase cofilin signaling pathway, greatly increasing GTPase RhoA activity.
      • $97
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    • AT13148
      T24821056901-62-2
      AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
      • $41
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    • URMC-099
      T60571229582-33-5
      URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
      • $52
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    • Ripasudil free base
      T7492223645-67-8
      Ripasudil free base (K-115 (free base)) is a selective and potent ROCK inhibitor, is a novel and potent antiglaucoma agent.
      • $73
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    • Verosudil
      T609241414854-42-4
      Verosudil (AR-12286) is a highly potent Rho kinase (ROCK) inhibitor with a Ki of 2 nM and 2 nM against ROCK1 and ROCK2, respectively. AR-12286 mitigates steroid-induced intraocular pressure in mice by decreasing intraocular pressure through enhanced outflow of aqueous humor via the trabecular meshwork.
      • $89
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    • Thiazovivin
      T21551226056-71-8
      Thiazovivin, a ROCK inhibitor (IC50: 0.5 μM), increases the survival rate of hESC.
      • $30
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    • LX7101
      T157981192189-69-7In house
      LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM).
      • $56
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    • CMPD101
      T14989865608-11-3
      CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2 3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. 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.
      • $60
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    • ROCK inhibitor-2
      T127461127308-52-4
      ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 17 nM and 2 nM, respectively.
      • $60
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    • SB-747651A Dihydrochloride
      T96521781882-72-1In house
      SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].
      • $67
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    • Afuresertib
      T19111047644-62-1
      Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.
      • $33
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    • ROCK-IN-2
      TQ0110867017-68-3
      ROCK-IN-2 (Azaindole 1) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.
      • $116
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    • CCG-222740
      T77641922098-69-8
      CCG-222740 is an inhibitor of Rho MRTF pathway
      • $41
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    • Fasudil hydrochloride
      T3060105628-07-7
      Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.
      • $35
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    • H-1152 dihydrochloride
      T35328871543-07-6In house
      H-1152 dihydrochloride (H-1152 2HCl) is a specific inhibitor of Rho-associated protein kinase (ROCK) with an IC50 of 12 nM and a Ki of 1.6 nM. H-1152 dihydrochloride inhibits PKA, PKC, PKG, Aurora A and CaMKII with IC50 values of 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
      • $58
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    • GSK269962A
      T3518850664-21-0
      GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
      • $36
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    • Y-33075 dihydrochloride
      T13384L173897-44-4
      Y-33075 dihydrochloride is a selective inhibitor of ROCK with an IC50 of 3.6 nM.
      • $38
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    • BDP5290
      T73011817698-21-7
      BDP5290 is a potent inhibitor of both ROCK and MRCK, with IC50 values of 5 nM for ROCK1, 50 nM for ROCK2, 10 nM for MRCKα, and 100 nM for MRCKβ.
      • $51
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    • Fasudil
      T1606103745-39-7
      Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
      • $33
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    • GSK180736A
      T3513817194-38-0
      GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).
      • $35
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    • GSK429286A
      T2633864082-47-3
      GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
      • $35
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    • GSK-25
      T4488874119-56-9
      GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).
      • $39
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    • Hydroxyfasudil
      T4276L105628-72-6
      Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).
      • $35
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    • Neoprzewaquinone A
      TN1985630057-39-5
      Neoprzewaquinone A (NEO), an active ingredient of S. miltiorrhiza, inhibits breast cancer cell migration and promotes smooth muscle relaxation by targeting PIM1 and blocking the ROCK2 STAT3 pathway.
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      • Hydroxyfasudil Hydrochloride
        T4276155558-32-0
        Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) is a ROCK1 2 inhibitor (IC50s: 0.73 0.72 μM).
        • $34
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      • Afuresertib hydrochloride
        T78851047645-82-8
        Afuresertib hydrochloride is an inhibitor of Akt kinase (Kis of 0.08 2 2.6 nM for Akt1 Akt2 Akt3 respectively)
        • $44
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      • RKI-1447
        T18981342278-01-6
        RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.
        • $47
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      • BDP9066
        T145212226507-04-4
        BDP9066 is a potent and selective MRCK inhibitor that inhibits MRCKβ and MRCKα β and can be used for the prevention and treatment of skin cancer.
        • $52
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      • SAR407899
        T7391923359-38-0
        SAR407899 is Rho kinase inhibitor potently inhibits endothelin-1-induced constriction of renal resistance arteries.
        • $33
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      • SR-3677
        TQ01871072959-67-1
        SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM).
        • $30
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      • ZINC00881524
        T4095557782-81-7
        ZINC00881524 (ROCK inhibitor) is an effective and specific ROCK inhibitor.
        • $29
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      • RKI1313
        T20111342276-76-9
        RKI1313 (RKI-1313) was a selective inhibitor for ROCK-dependent signaling, cytoskeletal changes, anchorage-independent colony formation, migration, and invasion.
        • $247
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      • CRT0066854 hydrochloride
        T108882250019-91-9In house
        CRT0066854 hydrochloride is an effective selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively.
        • $33
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      • CKI-7
        T199131177141-67-1
        CKI-7 is a potent, ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. It also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.
        • $116
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      • Belumosudil
        T6867911417-87-3
        Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50 Ki: 60 41 nM).
        • $41
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      • CID-5056270
        T23888681173-76-2In house
        CID-5056270 has anticancer activity and can inhibit lung cancer, anal cancer, bladder cancer, cervical cancer, vulvar cancer, penile cancer, Burkitt's lymphoma, breast cancer and bone cancer. It can be used to study hypertension, Alzheimer's disease and arteriosclerosis.
        • $329
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      • LX-7101 hydrochloride
        T329851374644-80-0In house
        LX-7101 hydrochloride is a potent LIMK and ROCK2 inhibitor with antihypertensive activity, inhibits LIMK1/2, ROCK, PKA, and can be used to study glaucoma.
        • $195
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      • GKI-1 HCl
        T11402L In house
        GKI-1 HCl is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL and hGWL-KinDom.The inhibitory effect of GKI-1 HCl on ROCK1 is more significant.
        • $161
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      • WAY-656935
        T77609852902-81-9
        WAY-656935 inhibits ROCK.
        • $45
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      • Rhodblock 6
        T26078886625-06-5
        Rhodblock 6 is a Rho kinase (ROCK) inhibitor that specifically inhibits Rho kinase activity and the localization of phosphorylated MRLC (Myosin Regulatory Light Chain).
        • $45
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      • ROCK-IN-5
        T67748692870-25-0In house
        ROCK-IN-5 (compound I-B-37) is a potent inhibitor of protein kinases, including ROCK, ERK, GSK, and AGC, with potential applications in cardiac, proliferative, and neurodegenerative disease research.
        • $38
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      • Rho-Kinase-IN-1
        T127211035094-83-7In house
        Rho-Kinase-IN-1 is an inhibitor of ROCK with Kis of 30.5 nM and 3.9 nM for ROCK1 and ROCK2, respectively. Rho-Kinase-IN-1 can be used in studies about excessive cell proliferation, remodeling, edema and inflammation diseases.
        • $68
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      • ROCK2-IN-2
        T127471995065-79-6
        ROCK2-IN-2 is a selective inhibitor of ROCK2, with an IC50 of less than 1 μM.
        • $48
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      • SAR407899 hydrochloride
        T23308923262-96-8
        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.
        • $29
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