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ROCK Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S1049 Y-27632 Dihydrochloride 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.
Genome Biol, 2026, 27(1)73
MedComm (2020), 2026, 7(3):e70656
Cell Commun Signal, 2026, 24(1)198
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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.
Stem Cell Res Ther, 2026, 17(1)109
Cancers (Basel), 2026, 18(5)827
Front Oncol, 2026, 16:1773072
S1573 Fasudil (HA-1077) Hydrochloride 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.
bioRxiv, March 20 2024, nan
Translational Vision Science & Technology, June 20 2017, 22
PeerJ, June 06 2023, e15494
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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.
Circulation, 2025, 397-415
Nucleic Acids Res, 2025, 53(12)gkaf539
Stem Cell Res, 2025, 87:103776
Verified customer review of Thiazovivin (TZV)
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
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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
S7195 RKI-1447 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.
Future Medicinal Chemistry, 2024, 873–885
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Pharmaceuticals (Basel), 2023, 16(2)294
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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.
Cells, May 3, 2023, 1307
Communications Medicine, April 19, 2023, 53
Mol Ther Nucleic Acids, 2025, 36(4):102758
S7936 KD025 (Belumosudil) 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.
Oncology Letters, September 30, 2020, 309
bioRxiv, September 20, 2024, 2024.09.16.613317
Clinical and Translational Medicine, October 2022, e1036
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.
Stem Cell Reports, 2024, 19(4):579-595
bioRxiv, 2024, 2024.01.09.574940
bioRxiv, 2024, 2023.05.04.538989
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
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.
Molecular Cancer Research, November 01 2023, 1205-1219
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. This compound also inhibits the activity of MRCK with IC50 of 150 nM.
E1480 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) 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.
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.
E2519 WAY-624704 WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM.
E0048New ROCK inhibitor-2 ROCK inhibitor-2 (compound 6) is a potent, selective dual inhibitor of ROCK1 and ROCK2 with IC50 of 160 nM and 21 nM, respectively. It exhibits antitumor by inhibiting cell migration and reducing cell-in-cell structure formation in U2OS cells.
E1921 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.
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
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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 Reports Medicine, August 2025, 102297
Cell Rep Med, 2025, 6(8):102297