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Catalog No. Product Name Information Product Use Citations Product Validations
E2519New WAY-624704 WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM.
S1049 Y-27632 2HCl Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Bioact Mater, 2023, 20:286-305
Nature, 2022, 603(7899):131-137
Nat Biotechnol, 2022, 10.1038/s41587-022-01219-z
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.
Stem Cell Res Ther, 2022, 13(1):158
Cell Prolif, 2022, 10.1111/cpr.13244
Int J Mol Sci, 2022, 23(7)4053
S1474 GSK429286A GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
Sci Rep, 2022, 12(1):7
FASEB J, 2020, 22
Carcinogenesis, 2020, 41(7):993-1004
S1573 Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877), 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.
Aging Cell, 2022, e13587
Cell Death Dis, 2022, 13(2):138
iScience, 2022, 25(6):104398
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic 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.
S6390 Y-27632 Y-27632 is a specific inhibitor of ROCK with an Ki of 140 nM for ROCK1 (p160ROCK). Y-27632 shows >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Bioact Mater, 2023, 20:286-305
Cell Res, 2022, 10.1038/s41422-022-00614-0
Mol Cell, 2022, S1097-2765(22)00442-7
S6636 Azaindole 1 (TC-S 7001) Azaindole 1 (TC-S 7001) 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.
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.
Sci Rep, 2022, 12(1):7
Cell Biosci, 2021, 11(1):105
Carcinogenesis, 2020, 41(7):993-1004
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.
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
Sci Rep, 2021, 11(1):18532
Cell, 2020, 182(3):685-712.e19
S7687 GSK269962A HCl GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
Cancer Discov, 2020, CD-20-0160
Elife, 2020, 9:e58165
Nat Commun, 2019, 10(1):1333
S7935 Y-39983 HCl Y-39983 HCl (Y-33075) is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
In Vitro Cell Dev Biol Anim, 2019, 55(4):260-271
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.
Sci Adv, 2022, 8(15):eabm3471
Nat Commun, 2022, 13(1):703
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
S7995 Ripasudil (K-115) hydrochloride dihydrate Ripasudil (K-115) hydrochloride dihydrate is 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.
FASEB J, 2022, 36(7):e22397
J Immunother Cancer, 2021, 9(1)e001481
Cell, 2020, 182(3):685-712.e19
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
S8226 Netarsudil (AR-13324) 2HCl Netarsudil (a.k.a. AR-13324) is 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.
S8448 ZINC00881524 (ROCK inhibitor) ZINC00881524 is a ROCK inhibitor.
Cancer Res, 2022, canres.2691.2021
Cell Prolif, 2022, e13211
Adv Mater, 2021, e2100096
E2519New WAY-624704 WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM.
S1049 Y-27632 2HCl Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Bioact Mater, 2023, 20:286-305
Nature, 2022, 603(7899):131-137
Nat Biotechnol, 2022, 10.1038/s41587-022-01219-z
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.
Stem Cell Res Ther, 2022, 13(1):158
Cell Prolif, 2022, 10.1111/cpr.13244
Int J Mol Sci, 2022, 23(7)4053
S1474 GSK429286A GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
Sci Rep, 2022, 12(1):7
FASEB J, 2020, 22
Carcinogenesis, 2020, 41(7):993-1004
S1573 Fasudil (HA-1077) HCl Fasudil (HA-1077, AT-877), 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.
Aging Cell, 2022, e13587
Cell Death Dis, 2022, 13(2):138
iScience, 2022, 25(6):104398
S3233 Emetine hydrochloride Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic 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.
S6390 Y-27632 Y-27632 is a specific inhibitor of ROCK with an Ki of 140 nM for ROCK1 (p160ROCK). Y-27632 shows >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
Bioact Mater, 2023, 20:286-305
Cell Res, 2022, 10.1038/s41422-022-00614-0
Mol Cell, 2022, S1097-2765(22)00442-7
S6636 Azaindole 1 (TC-S 7001) Azaindole 1 (TC-S 7001) 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.
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.
Sci Rep, 2022, 12(1):7
Cell Biosci, 2021, 11(1):105
Carcinogenesis, 2020, 41(7):993-1004
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.
Br J Cancer, 2021, 10.1038/s41416-021-01442-6
Sci Rep, 2021, 11(1):18532
Cell, 2020, 182(3):685-712.e19
S7687 GSK269962A HCl GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
Cancer Discov, 2020, CD-20-0160
Elife, 2020, 9:e58165
Nat Commun, 2019, 10(1):1333
S7935 Y-39983 HCl Y-39983 HCl (Y-33075) is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.
Cell, 2020, 182(3):685-712.e19
Cell, 2020, 182(3):685-712.e19
In Vitro Cell Dev Biol Anim, 2019, 55(4):260-271
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.
Sci Adv, 2022, 8(15):eabm3471
Nat Commun, 2022, 13(1):703
ACS Chem Biol, 2022, 10.1021/acschembio.2c00052
S7995 Ripasudil (K-115) hydrochloride dihydrate Ripasudil (K-115) hydrochloride dihydrate is 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.
FASEB J, 2022, 36(7):e22397
J Immunother Cancer, 2021, 9(1)e001481
Cell, 2020, 182(3):685-712.e19
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
S8226 Netarsudil (AR-13324) 2HCl Netarsudil (a.k.a. AR-13324) is 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.
S8448 ZINC00881524 (ROCK inhibitor) ZINC00881524 is a ROCK inhibitor.
Cancer Res, 2022, canres.2691.2021
Cell Prolif, 2022, e13211
Adv Mater, 2021, e2100096
E2519New WAY-624704 WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM.
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