ROCK Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Neoplasia, 2023, 10.1016/j.neo.2023.100948
Pharmaceuticals (Basel), 2023, 16(2)294
Sci Rep, 2022, 12(1):7
Verified customer review of RKI-1447
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
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. 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 fibre formation and inhibits migration and invasion of multiple cancer cell line
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) 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 an antifibrotic effect.
E2519 WAY-624704 WAY-624704 is a novel Rho kinases (ROCK) inhibitor with a Ki of 17 nM.
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
Verified customer review of AT13148
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