ROCK

亜型選択性的な製品

ROCK製品

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  • ROCK阻害剤 (19)
  • 新製品
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S1049 Y-27632 Dihydrochloride Y-27632 2HCl は選択的 ROCK1 (p160ROCK) 阻害剤であり、cell-free assay における Ki は 140 nM です。PKC, cAMP-依存性プロテインキナーゼ, MLCK や PAK など他のキナーゼよりも ROCK1 に対して 200 倍以上の選択性を示します。
Cell, 2025, S0092-8674(25)00406-4
Cell, 2025, S0092-8674(25)00807-4
Cancer Cell, 2025, S1535-6108(25)00262-4
Y-27632-S1049Y0220150625.gif
S6390 Y-27632 Y-27632 is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Science, 2025, 388(6747):eadk3487
Nat Biotechnol, 2025, 10.1038/s41587-025-02833-3
Circulation, 2025, 151(20):1436-1448
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Transl Oncol, 2025, 51:102209
J Immunother Cancer, 2024, 12(11)e009805
Sci China Life Sci, 2024, 67(8):1549-1562
fasudil-S157301W0120140228.gif
S1459 Thiazovivin (TZV) Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation.
Nucleic Acids Res, 2025, 53(12)gkaf539
Nucleic Acids Res, 2025, 53(12)gkaf539
Stem Cell Res, 2025, 87:103776
Thiazovivin-S145901Y0120140126.gif
S1474 GSK429286A GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
iScience, 2023, 26(12):108532
Sci Rep, 2022, 12(1):7
Cancer Sci, 2020, 112(1):133-143
GSK429286A-S147401W0120140228.gif
S8448 ZINC00881524 (ROCK inhibitor) ZINC00881524 is a ROCK inhibitor.
bioRxiv, 2023, 2023.06.07.544100
Nat Commun, 2022, 13(1):7171
Cancer Res, 2022, canres.2691.2021
S7563 AT13148 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.
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Cancers (Basel), 2022, 14(23)5943
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
AT13148-S756301Z0120161118.gif
S7195 RKI-1447 RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities.
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Pharmaceuticals (Basel), 2023, 16(2)294
Sci Rep, 2022, 12(1):7
RKI-1447-S719501Z0220161125.gif
S7936 Belumosudil (KD025) Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.
Zool Res, 2024, 45(3):535-550
bioRxiv, 2024, 2024.09.16.613317
Commun Biol, 2023, 10.1038/s42003-023-05552-0
S7687 GSK269962A HCl GSK269962A HClは一種の選択性的なROCK阻害剤で、ROCK1とROCK2に作用する時のIC50値が1.6nMと4nMに分かれることです。
Stem Cell Reports, 2024, 19(4):579-595
bioRxiv, 2024, 2024.01.09.574940
bioRxiv, 2024, 2024.01.09.574940
S7935 Y-39983 Dihydrochloride Y-39983 (Y-33075) Dihydrochloride is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.
iScience, 2024, 27(12):111434
Sci Rep, 2024, 14(1):30786
Cells, 2023, 12(9)1307
S8226 Netarsudil (AR-13324) 2HCl Netarsudil (AR-13324) is a ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension.
Cells, 2025, 14(4)258
Virulence, 2025, 16(1):2489751
Exp Eye Res, 2025, 255:110351
S8208 Hydroxyfasudil HCl 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.
Commun Med (Lond), 2025, 5(1):129
Eur J Pharmacol, 2024, 979:176835
bioRxiv, 2020, 10.1101/2020.11.26.393801
F0409 ROCK1 Antibody [L9K19] ROCK1 Rabbit mAb recognizes endogenous levels of total ROCK1 protein.
iScience, 2024, 27(2):108969
F1209 ROCK2 Antibody [K12H24] ROCK2 Rabbit mAb recognizes endogenous levels of total ROCK2 protein.
E1261 Chroman 1 Chroman 1 is a highly potent and selective ROCK inhibitor with IC50 of 1 pM and 52 pM against ROCK2 and ROCK1, respectively. Chroman 1 also inhibits the activity of MRCK with IC50 of 150 nM.
S7512 GSK269962A 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.
S6636 Azaindole 1 (BAY-549) Azaindole 1 (BAY-549) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 nM and 1.1 nM for human ROCK1 and ROCK2 in an ATP-competitive manner.
E1978 Zelasudil Zelasudil (RXC007) is a selective inhibitor of Rho-associated coiled-coil-containing kinase 2 (ROCK2). It has been found to have the antifibrotic effect.
S6214 H-1152 dihydrochloride 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.
Cell Rep Med, 2025, 6(8):102297
E1921New NRL-1049 NRL-1049(BA 1049) is a small molecule selective inhibitor of ROCK2 with an IC50 of 0.59 µM. It exhibits potent efficacy in preserving the blood-brain barrier (BBB) and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice.
S1049 Y-27632 Dihydrochloride Y-27632 2HCl は選択的 ROCK1 (p160ROCK) 阻害剤であり、cell-free assay における Ki は 140 nM です。PKC, cAMP-依存性プロテインキナーゼ, MLCK や PAK など他のキナーゼよりも ROCK1 に対して 200 倍以上の選択性を示します。
Cell, 2025, S0092-8674(25)00406-4
Cell, 2025, S0092-8674(25)00807-4
Cancer Cell, 2025, S1535-6108(25)00262-4
Y-27632-S1049Y0220150625.gif
S6390 Y-27632 Y-27632 is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Science, 2025, 388(6747):eadk3487
Nat Biotechnol, 2025, 10.1038/s41587-025-02833-3
Circulation, 2025, 151(20):1436-1448
S1573 Fasudil HCl Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Transl Oncol, 2025, 51:102209
J Immunother Cancer, 2024, 12(11)e009805
Sci China Life Sci, 2024, 67(8):1549-1562
fasudil-S157301W0120140228.gif
S1459 Thiazovivin (TZV) Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation.
Nucleic Acids Res, 2025, 53(12)gkaf539
Nucleic Acids Res, 2025, 53(12)gkaf539
Stem Cell Res, 2025, 87:103776
Thiazovivin-S145901Y0120140126.gif
S1474 GSK429286A GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
iScience, 2023, 26(12):108532
Sci Rep, 2022, 12(1):7
Cancer Sci, 2020, 112(1):133-143
GSK429286A-S147401W0120140228.gif
S8448 ZINC00881524 (ROCK inhibitor) ZINC00881524 is a ROCK inhibitor.
bioRxiv, 2023, 2023.06.07.544100
Nat Commun, 2022, 13(1):7171
Cancer Res, 2022, canres.2691.2021
S7563 AT13148 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.
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Cancers (Basel), 2022, 14(23)5943
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
AT13148-S756301Z0120161118.gif
S7195 RKI-1447 RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities.
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Pharmaceuticals (Basel), 2023, 16(2)294
Sci Rep, 2022, 12(1):7
RKI-1447-S719501Z0220161125.gif
S7936 Belumosudil (KD025) Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.
Zool Res, 2024, 45(3):535-550
bioRxiv, 2024, 2024.09.16.613317
Commun Biol, 2023, 10.1038/s42003-023-05552-0
S7687 GSK269962A HCl GSK269962A HClは一種の選択性的なROCK阻害剤で、ROCK1とROCK2に作用する時のIC50値が1.6nMと4nMに分かれることです。
Stem Cell Reports, 2024, 19(4):579-595
bioRxiv, 2024, 2024.01.09.574940
bioRxiv, 2024, 2024.01.09.574940
S7935 Y-39983 Dihydrochloride Y-39983 (Y-33075) Dihydrochloride is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.
iScience, 2024, 27(12):111434
Sci Rep, 2024, 14(1):30786
Cells, 2023, 12(9)1307
S8226 Netarsudil (AR-13324) 2HCl Netarsudil (AR-13324) is a ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension.
Cells, 2025, 14(4)258
Virulence, 2025, 16(1):2489751
Exp Eye Res, 2025, 255:110351
S8208 Hydroxyfasudil HCl 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.
Commun Med (Lond), 2025, 5(1):129
Eur J Pharmacol, 2024, 979:176835
bioRxiv, 2020, 10.1101/2020.11.26.393801
E1261 Chroman 1 Chroman 1 is a highly potent and selective ROCK inhibitor with IC50 of 1 pM and 52 pM against ROCK2 and ROCK1, respectively. Chroman 1 also inhibits the activity of MRCK with IC50 of 150 nM.
S7512 GSK269962A 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.
S6636 Azaindole 1 (BAY-549) Azaindole 1 (BAY-549) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 nM and 1.1 nM for human ROCK1 and ROCK2 in an ATP-competitive manner.
E1978 Zelasudil Zelasudil (RXC007) is a selective inhibitor of Rho-associated coiled-coil-containing kinase 2 (ROCK2). It has been found to have the antifibrotic effect.
S6214 H-1152 dihydrochloride 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.
Cell Rep Med, 2025, 6(8):102297
E1921New NRL-1049 NRL-1049(BA 1049) is a small molecule selective inhibitor of ROCK2 with an IC50 of 0.59 µM. It exhibits potent efficacy in preserving the blood-brain barrier (BBB) and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice.
E1921New NRL-1049 NRL-1049(BA 1049) is a small molecule selective inhibitor of ROCK2 with an IC50 of 0.59 µM. It exhibits potent efficacy in preserving the blood-brain barrier (BBB) and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice.

ROCKシグナル伝達経路