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ROCK

Items 1-50 of 103

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Catalog No.
Product Name
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Product Information
Citations
  1. A15225
    Azaindole 1 (BAY-549)

    ROCK inhibitor

    Azaindole 1 (BAY-549) is a highly potent inhibitor of human ROCK-1 and ROCK-2 isoenzymes with IC50 values of 0.6 and 1.1 nM, respectively.

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  2. A10381
    Fasudil HCl (HA-1077)

    ROCK inhibitor

    Fasudil HCl is a cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM).
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  3. A12348
    GSK 269962

    ROCK inhibitor

    GSK 269962 is a potent Rho kinase (ROCK) inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively).
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  4. A21448
    Y-27632

    ROCK-I/ROCK-II inhibitor

    Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.
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  5. A15888
    Ripasudil

    ROCK inhibitor

    Ripasudil (K-115) is potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.
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  6. A11001
    Y-27632 2HCl

    ROCK Inhibitor

    Y-27632 is a Rho-Associated Coil Kinase (ROCK) inhibitor that increases the cloning efficiency of human embryonic stem cells (hESCs).
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  7. A12464
    AT13148

    multi-AGC kinase inhibitor

    AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors.
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  8. A12674
    SR 3677

    ROCK inhibitor

    SR 3677  is a potent and selective Rho-kinase inhibitor (IC50 values are 3 and 56 nM for ROCK-II and ROCK-I respectively).

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  9. A13067
    RKI-1447

    ROCK1/ROCK2 inhibitor

    RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.
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  10. A11610
    Y-33075

    ROCK inhibitor

    Y-33075 is ROCK (Rho-associated coiled coil-forming protein kinase) inhibitor.
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  11. A11611
    Y-33075 dihydrochloride

    ROCK inhibitor

    Y-33075 dihydrochloride is a selective ROCK inhibitor with an IC50 of 3.6 nM.
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  12. A13659
    Glycyl-H 1152 2HCl

    ROCK inhibitor

    Glycyl-H 1152 2HCl is a selective and potent ROCK inhibitor (IC50 values are 0.0118, 2.35, 2.57, 3.26, > 10 and >10 uM for ROCKII, Aurora A, CAMKII, PKG, PKA and PKC respectively.)
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  13. A13785
    HA-1077 dihydrochloride

    ROCK Inhibitor

    HA-1077 inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist.
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  14. A15921
    SAR407899 HCl

    ROCK inhibitor

    SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity.
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  15. A16966
    BDP5290

    ROCK and MRCK inhibitor

    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.
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  16. A20736
    GSK180736A

    GRK2 inhibitor

    GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
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  17. A19795
    CMPD101

    GRK2/GRK3 inhibitor

    CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively).
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  18. A20062
    ROCK2-IN-2

    ROCK2 inhibitor

    ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM.
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  19. A20090
    SB-772077B dihydrochloride

    ROCK inhibitor

    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.
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  20. A20403
    Rho-Kinase-IN-1

    ROCK inhibitor

    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.
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  21. A20477
    ZINC00881524

    ROCK inhibitor

    ZINC00881524 is a ROCK inhibitor.
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  22. A18912
    ROCK inhibitor-2

    ROCK1/ROCK2 inhibitor

    ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively.
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  23. A15045
    chroman 1

    ROCK Inhibitor

    Chroman 1 is a highly potent and selective ROCK II inhibitor.
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  24. A15101
    H-1152

    ROCK inhibitor

    H-1152, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases.
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  25. A15102
    H-1152 dihydrochloride

    ROCK inhibitor

    H-1152 dihydrochloride, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases.
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  26. A15118
    Hydroxyfasudil

    ROCK inhibitor

    Hydroxyfasudil, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.
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  27. A15119
    Hydroxyfasudil hydrochloride

    ROCK inhibitor

    Hydroxyfasudil hydrochloride, metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.
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  28. A15178
    Narciclasine

    ROCK activator

    Narciclasine is a Rho/Rho kinase/LIM kinase/cofilin signaling pathway activator.
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  29. A15226
    ROCK inhibitor-1

    ROCK inhibitor

    N/A
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  30. A15239
    SLx-2119 (KD025)

    ROCK2 Inhibitor

    SLx-2119 is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM).
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  31. A30863
    RKI-1447 dihydrochloride

    ROCK Inhibitor

    RKI-1447 dihydrochloride is a selective inhibitor of Rho-associated kinase (ROCK), exhibiting IC50 values of 14.5 nM and 6.2 nM for ROCK1 and ROCK2, respectively. This compound effectively suppresses the growth of colorectal carcinoma cells while inducing apoptosis, making it a valuable tool for research in cancer biology and therapeutics targeting ROCK signaling pathways.
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  32. A36696
    ROCK-IN-5

    ROCK/ERK/GSK/AGC Inhibitor

    ROCK-IN-5 (compound I-B-37) is a potent inhibitor of Rho-associated protein kinase (ROCK), as well as ERK, GSK-3, and AGC protein kinases. This compound exhibits significant biological activity in regulating cellular proliferation and has applications in researching cardiac conditions and neurodegenerative diseases. Its broad inhibitory profile makes it a valuable tool for studies aimed at understanding signaling pathways involved in various disease mechanisms.
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  33. A36792
    NRL-1049 dihydrochloride

    ROCK2 Inhibitor

    NRL-1049 dihydrochloride is a selective inhibitor of rho-associated protein kinase 2 (ROCK2), exhibiting an IC50 value of 0.59 μM. This compound demonstrates a remarkable selectivity for ROCK2 over ROCK1, with an IC50 of 26 μM, effectively inhibiting ROCK2 activity. NRL-1049 dihydrochloride has significant potential in research applications focused on the preservation of the blood-brain barrier following acute injury.
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  34. A36793
    Zelasudil

    ROCK Inhibitor

    Zelasudil is a selective inhibitor of Rho-associated coiled-coil containing protein kinase 2 (ROCK2), demonstrating significant anti-fibrotic activity. This small molecule enhances immunomodulatory responses in metastatic pancreatic tumors, promoting increased infiltration of CD8+ and CD4+ T cells while reducing FOXP3+ regulatory T cells at the tumor periphery. Zelasudil shows potential for advancing research in pancreatic ductal adenocarcinoma and related therapeutic strategies.
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  35. A36794
    Netarsudil

    ROCK/NET Inhibitor

    Netarsudil functions as a competitive inhibitor of Rho-associated protein kinases (ROCK I and ROCK II) and a reversible inhibitor of the norepinephrine transporter (NET). This compound effectively reduces intraocular pressure through ROCK inhibition, promoting relaxation of trabecular meshwork cells and dilation of episcleral veins, facilitating aqueous humor outflow while simultaneously decreasing aqueous humor production via NET inhibition. Netarsudil is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma.
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  36. A36795
    Belumosudil mesylate

    ROCK2 Inhibitor

    Belumosudil mesylate is a selective inhibitor of the Rho-associated kinase 2 (ROCK2), demonstrating an IC50 of 105 nM for ROCK2 and 24 µM for ROCK1. This compound exhibits significant anti-fibrotic properties, making it valuable for research in fibrosis-related pathways and diseases. Belumosudil mesylate is applicable in studies aimed at understanding the role of ROCK signaling in various physiological and pathological processes.
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  37. A36796
    SAR407899

    ROCK Inhibitor

    SAR407899 is a selective and potent ROCK inhibitor that acts competitively with ATP, exhibiting an IC50 of 135 nM for ROCK-2 and Kis of 36 nM in human and 41 nM in rat ROCK-2. This compound demonstrates stable inhibition of migrasome formation and is valuable for research into cellular migration and related processes. Its application in studies of ROCK signaling pathways may enhance the understanding of various physiological and pathological conditions.
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  38. A36797
    Netarsudil dimesylate

    ROCK/NET Inhibitor

    Netarsudil dimesylate is a potent inhibitor of Rho-associated kinases (ROCK I and ROCK II) and also serves as a reversible inhibitor of the norepinephrine transporter (NET). It effectively reduces intraocular pressure through ROCK inhibition, leading to the relaxation of trabecular meshwork cells and dilation of episcleral veins, which facilitates aqueous humor outflow, while simultaneously inhibiting NET to diminish aqueous humor production. This compound is primarily utilized in research related to ocular hypertension and primary open-angle glaucoma.
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  39. A36800
    Sovesudil

    ROCK Inhibitor

    Sovesudil is a potent Rho kinase (ROCK) inhibitor that functions through ATP-competitive mechanisms, exhibiting IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II. It effectively lowers intraocular pressure (IOP) while minimizing the risk of hyperemia, making it a valuable compound for ocular research and potential therapeutic applications in glaucoma treatment and other related conditions.
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  40. A36802
    Verosudil

    ROCK Inhibitor

    Verosudil is a potent Rho-associated protein kinase (ROCK) inhibitor, demonstrating robust inhibitory activity against both ROCK1 and ROCK2 with a Ki value of 2 nM. Its relatively lower selectivity for other kinases such as PKA, PKCT, MRCKA, and CAMK2A provides additional research avenues. Verosudil enhances trabecular outflow capacity, making it a valuable reagent in studies targeting intraocular pressure reduction. This compound is particularly relevant for research focused on glaucoma and ocular hypertension.
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  41. A36803
    3-(4-Pyridyl)indole

    ROCK Inhibitor

    3-(4-Pyridyl)indole is a selective Rho-kinase (ROCK) inhibitor, exhibiting an IC50 value of 25 μM. This compound is known to effectively inhibit cellular blebbing and promote the dissolution of actin stress fibers, making it a valuable reagent for studying wound healing mechanisms and cytoskeletal dynamics in various biological research applications.
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  42. A36804
    GSK269962A hydrochloride

    ROCK Inhibitor

    GSK269962A hydrochloride is a potent ROCK inhibitor that selectively targets Rho-associated coiled-coil kinase 1 (ROCK1) and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively. It exhibits significant anti-inflammatory and vasodilatory properties, making it valuable in research applications focused on vascular biology, cardiovascular diseases, and inflammatory conditions. This compound provides a useful tool for elucidating the role of ROCK signaling in various biological processes.
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  43. A36805
    CAY10746

    ROCK Inhibitor

    CAY10746 is a selective inhibitor of Rho-associated protein kinase (ROCK), demonstrating potent inhibitory activity against ROCK I and ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. This compound is particularly relevant for research into diabetic retinopathy (DR) and other conditions associated with abnormal vascular function. Its ability to modulate ROCK activity makes it a valuable tool in studying cellular pathways involved in inflammation and tissue remodeling.
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  44. A36806
    (rac)-AR-13503

    ROCK/PKC Inhibitor

    (rac)-AR-13503 is a potent inhibitor of Rho-associated protein kinase (ROCK) and protein kinase C (PKC). It plays a significant role in regulating angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. Additionally, (rac)-AR-13503 has demonstrated the ability to inhibit aberrant neovascularization in the oxygen-induced retinopathy (OIR) model in mice, making it a valuable tool for research in ocular disorders and vascular biology.
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  45. A36807
    Rho-Kinase-IN-2

    ROCK Inhibitor

    Rho-Kinase-IN-2 is a selective inhibitor of Rho Kinase (ROCK) with an IC50 value of 3 nM for ROCK2. This orally active and CNS-permeable compound is significant for investigating the role of ROCK in neurodegenerative disorders, particularly Huntington's disease. Its potent inhibition of this pathway makes it a valuable tool for exploring therapeutic strategies targeting ROCK activity in relevant biological models.
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  46. A36808
    Sovesudil hydrochloride

    ROCK Inhibitor

    Sovesudil hydrochloride is a highly selective Rho kinase (ROCK) inhibitor that competitively binds to ATP, demonstrating IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II. It effectively reduces intraocular pressure (IOP) and is noteworthy for its ability to do so without causing hyperemia. This compound is utilized in research focused on glaucoma and other ocular conditions linked to elevated IOP.
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  47. A36809
    ROCK2-IN-6 hydrochloride

    ROCK2 Inhibitor

    ROCK2-IN-6 hydrochloride is a selective inhibitor of Rho-associated protein kinase 2 (ROCK2). It modulates ROCK2 activity, making it a valuable tool for studying disorders associated with ROCK signaling, including autoimmune diseases and inflammation. This compound is ideal for research aimed at understanding the role of ROCK2 in various biological processes and therapeutic interventions.
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  48. A36810
    ROCK2-IN-8

    ROCK2 Inhibitor

    ROCK2-IN-8 is an orally active inhibitor of Rho-associated protein kinase 2 (ROCK2) with an IC50 of 7.2 nM. This compound is valuable in studies investigating aqueous humor outflow in porcine eyes, as well as the phosphorylation of myosin light chain. Its specificity for ROCK2 makes it a useful tool in exploring the roles of this kinase in various biological processes.
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  49. A36812
    GSK-25

    ROCK1 Inhibitor

    GSK-25 is a potent and selective inhibitor of ROCK1, demonstrating an IC50 of 7 nM. This compound exhibits excellent selectivity against a diverse panel of 31 kinases, with over 100-fold selectivity compared to RSK1 (IC50 = 398 nM) and p70S6K (IC50 = 1 µM). GSK-25 is also characterized by its inhibitory effects on specific cytochrome P450 enzymes, with IC50 values of 2.5 µM, 5.2 µM, and 2.5 µM for CYP2C9, CYP2D6, and CYP3A4, respectively. This makes GSK-25 suitable for research applications focused on cell signaling and pharmacological studies involving the ROCK pathway.
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  50. A36813
    ROCK1-IN-1

    ROCK1 Inhibitor

    ROCK1-IN-1 is a selective ROCK1 inhibitor with a Ki value of 540 nM. This compound is utilized in research focused on hypertension, glaucoma, and erectile dysfunction by modulating the Rho-associated protein kinase pathway. Its inhibition of ROCK1 activity provides insight into various physiological processes and potential therapeutic interventions for related disorders.
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