ROCK

Isoform-selective Products

Signaling Pathway

ROCK Signaling Pathway

ROCK Products

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  • ROCK Inhibitors (19)
  • New ROCK Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1049 Y-27632 2HCl Y-27632 2HCl 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.
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
S7995 Ripasudil hydrochloride dihydrate Ripasudil hydrochloride dihydrate is a 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.
Elife, 2023, 12e80254
bioRxiv, 2023, 10.1101/2023.04.03.535438
FASEB J, 2022, 36(7):e22397
S7687 GSK269962A HCl 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.
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.
E1480New DJ4 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 fiber formation and inhibits migration and invasion of multiple cancer cell line
S6636 Azaindole 1 (BAY-549) Azaindole 1 (BAY-549) 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.
E2519 WAY-624704 WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM.
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 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.
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
S7995 Ripasudil hydrochloride dihydrate Ripasudil hydrochloride dihydrate is a 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.
Elife, 2023, 12e80254
bioRxiv, 2023, 10.1101/2023.04.03.535438
FASEB J, 2022, 36(7):e22397
S7687 GSK269962A HCl 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.
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.
E1480New DJ4 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 fiber formation and inhibits migration and invasion of multiple cancer cell line
S6636 Azaindole 1 (BAY-549) Azaindole 1 (BAY-549) 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.
E2519 WAY-624704 WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM.
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.
E1480New DJ4 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 fiber formation and inhibits migration and invasion of multiple cancer cell line

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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