ROCK

亜型選択性的な製品

シグナル伝達経路

ROCKシグナル伝達経路

ROCK製品

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  • ROCK阻害剤 (16)
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S1049 Y-27632 2HCl 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。
Nature, 2024, 10.1038/s41586-024-07067-y
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):827
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.
Adv Sci (Weinh), 2024, 11(3):e2304303
Cell Rep Med, 2024, 5(2):101396
Acta Biomater, 2024, S1742-7061(24)00036-9
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.
PeerJ, 2023, 11:e15494
Alcohol, 2023, 115:5-12
medRxiv, 2023, 10.1101/2023.12.19.23299785
S1459 Thiazovivin Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation.
Cell Mol Life Sci, 2024, 81(1):92
iScience, 2024, 27(1):108599
Mol Ther Methods Clin Dev, 2024, 32(1):101204
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
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
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
Sci Rep, 2022, 12(1):7
Cell Biosci, 2021, 11(1):105
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.
Commun Biol, 2023, 10.1038/s42003-023-05552-0
Nat Commun, 2022, 13(1):703
Clin Transl Med, 2022, 12(10):e1036
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。
bioRxiv, 2023, 2023.05.04.538989
Cancer Discov, 2020, CD-20-0160
Elife, 2020, 9:e58165
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.
Cells, 2023, 12(9)1307
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
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.
Int J Mol Sci, 2023, 24(6)5464
S8208 Hydroxyfasudil (HA-1100) HCl Hydroxyfasudil (HA-1100), 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.
bioRxiv, 2020, 10.1101/2020.11.26.393801
E1261New 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.
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.
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.
S1049 Y-27632 2HCl 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。
Nature, 2024, 10.1038/s41586-024-07067-y
Nat Commun, 2024, 15(1):1285
Nat Commun, 2024, 15(1):827
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.
Adv Sci (Weinh), 2024, 11(3):e2304303
Cell Rep Med, 2024, 5(2):101396
Acta Biomater, 2024, S1742-7061(24)00036-9
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.
PeerJ, 2023, 11:e15494
Alcohol, 2023, 115:5-12
medRxiv, 2023, 10.1101/2023.12.19.23299785
S1459 Thiazovivin Thiazovivin is a novel ROCK inhibitor with IC50 of 0.5 μM in a cell-free assay, promotes hESC survival after single-cell dissociation.
Cell Mol Life Sci, 2024, 81(1):92
iScience, 2024, 27(1):108599
Mol Ther Methods Clin Dev, 2024, 32(1):101204
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
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
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
Sci Rep, 2022, 12(1):7
Cell Biosci, 2021, 11(1):105
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.
Commun Biol, 2023, 10.1038/s42003-023-05552-0
Nat Commun, 2022, 13(1):703
Clin Transl Med, 2022, 12(10):e1036
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。
bioRxiv, 2023, 2023.05.04.538989
Cancer Discov, 2020, CD-20-0160
Elife, 2020, 9:e58165
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.
Cells, 2023, 12(9)1307
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
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.
Int J Mol Sci, 2023, 24(6)5464
S8208 Hydroxyfasudil (HA-1100) HCl Hydroxyfasudil (HA-1100), 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.
bioRxiv, 2020, 10.1101/2020.11.26.393801
E1261New 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.
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.
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.
E1261New 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.

ROCK阻害剤の選択性比較

Tags: ROCK inhibition | ROCK activity | ROCK activation | Rho kinase inhibition | Rho kinase activation | Rho kinase activity | ROCK phosphorylation | ROCK signaling pathway | Rho kinase assay | Rho kinase signaling pathway | ROCK inhibitors for glaucoma | ROCK inhibitor review