| S7195 |
RKI-1447
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RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, and has anti-invasive and antitumor activities.
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Neoplasia, 2023, 10.1016/j.neo.2023.100948
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Pharmaceuticals (Basel), 2023, 16(2)294
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Sci Rep, 2022, 12(1):7
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| S7687 |
GSK269962A HCl
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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.
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Stem Cell Reports, 2024, 19(4):579-595
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bioRxiv, 2024, 2024.01.09.574940
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bioRxiv, 2024, 2023.05.04.538989
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| S7935 |
Y-39983 Dihydrochloride
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Y-39983 (Y-33075)Dihydrochloride is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.
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iScience, 2024, 27(12):111434
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Sci Rep, 2024, 14(1):30786
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Cells, 2023, 12(9)1307
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| S8208 |
Hydroxyfasudil HCl
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Hydroxyfasudil HCl, an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively.
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Commun Med (Lond), 2025, 5(1):129
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Eur J Pharmacol, 2024, 979:176835
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bioRxiv, 2020, 10.1101/2020.11.26.393801
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| E1261 |
Chroman 1
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Chroman 1 is a highly potent and selective ROCK inhibitor with IC50 of 1 pM and 52 pM against ROCK2 and ROCK1, respectively. This compound also inhibits the activity of MRCK with IC50 of 150 nM.
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| E1480 |
DJ4
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DJ4 (EX-A7863) is a potent, selective ATP-competitive inhibitor of ROCK1/2 and MRCKα/β with IC50 of 5/50 nM and 10/100 nM respectively. It blocks stress fibre formation and inhibits migration and invasion of multiple cancer cell line
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| S7512 |
GSK269962A
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GSK269962A is a potent and selective inhibitor of ROCK with IC50 values of 1.6 nM for ROCK1 and 4 nM for ROCK2. It shows potential as an alternative treatment for overactive bladder (OAB), and also exhibits anti-inflammatory and vasodilatory activities.
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| S6636 |
Azaindole 1 (BAY-549)
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BAY-549 (Azaindole 1) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner.
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| E1978 |
Zelasudil
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Zelasudil (RXC007) is a selective inhibitor of Rho-associated coiled-coil-containing kinase 2 (ROCK2). It has been found to have an antifibrotic effect.
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| E2519 |
WAY-624704
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WAY-624704 is a novel Rho kinases (ROCK) inhibitor with a Ki of 17 nM.
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| S7563 |
AT13148
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AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.
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Neoplasia, 2023, 10.1016/j.neo.2023.100948
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Cancers (Basel), 2022, 14(23)5943
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Br J Cancer, 2021, 10.1038/s41416-021-01442-6
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| S6214 |
H-1152 dihydrochloride
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H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
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Cell Rep Med, 2025, 6(8):102297
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