ROCK

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
Nature, 2022, 603(7899):131-137
Nat Biotechnol, 2022, 10.1038/s41587-022-01219-z
Cell, 2022, 185(5):794-814.e30
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.
S6390New 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.
Cell Res, 2022, 10.1038/s41422-022-00614-0
Mol Cell, 2022, S1097-2765(22)00442-7
Adv Sci (Weinh), 2022, e2106075
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.
J Immunother Cancer, 2021, 9(1)e001481
Cell, 2020, 182(3):685-712.e19
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
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.
Nature, 2022, 603(7899):131-137
Nat Biotechnol, 2022, 10.1038/s41587-022-01219-z
Cell, 2022, 185(5):794-814.e30
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.
S6390New 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.
Cell Res, 2022, 10.1038/s41422-022-00614-0
Mol Cell, 2022, S1097-2765(22)00442-7
Adv Sci (Weinh), 2022, e2106075
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.
J Immunother Cancer, 2021, 9(1)e001481
Cell, 2020, 182(3):685-712.e19
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
S6390New 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.
Cell Res, 2022, 10.1038/s41422-022-00614-0
Mol Cell, 2022, S1097-2765(22)00442-7
Adv Sci (Weinh), 2022, e2106075
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