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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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  • 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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  • Chroman 1
    T149601273579-40-0In house
    Chroman 1 is an inhibitor of ROCK2 (IC50: 1 nM).
    • $70
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  • Netarsudil Dihydrochloride
    T103581253952-02-1
    Netarsudil Dihydrochloride (AR-13324 Dihydrochloride) is an inhibitor of Rho-related protein kinase (ROCK) and norepinephrine transporter (NET) and is effective in reducing intraocular pressure (IOP).
    • $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
    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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    • 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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    • Netarsudil mesylate
      T10358L21422144-42-0
      Netarsudil mesylate (AR-13324 mesylate) is a Rho-related protein kinase inhibitor used to study glaucoma and hypertension.
      • $328
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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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    • 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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    • CCG-222740
      T77641922098-69-8
      CCG-222740 is an inhibitor of Rho MRTF pathway
      • $35
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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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    • 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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    • 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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    • 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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    • Fasudil
      T1606103745-39-7
      Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.
      • $33
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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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    • 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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    • 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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    • GSK429286A
      T2633864082-47-3
      GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
      • $35
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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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    • 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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    • 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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    • 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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    • AS 1892802
      T22037928320-12-1
      AS 1892802 is a potent and selective inhibitor of ROCK. AS 1892802 exibits IC50 values of 52nM, 57nM and 122 nM for human ROCK2, rat ROCK2 and human ROCK1, respectively. The onset of antinociceptive effect of AS 1892802 is as fast as those of Tramadol and Diclofenac.
      • $44
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    • SAR407899
      T7391923359-38-0
      SAR407899 is Rho kinase inhibitor potently inhibits endothelin-1-induced constriction of renal resistance arteries.
      • $31
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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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    • 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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    • 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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    • 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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    • 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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    • 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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    • WAY-656935
      T77609852902-81-9
      WAY-656935 inhibits ROCK.
      • $45
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