ROCK

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

ROCK Products

Catalog No. 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.

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.

S1573

Fasudil (HA-1077) HCl

Fasudil(HA-1077), 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.

S1474

GSK429286A

GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

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.

S3239New

Emetine Dihydrochloride

Emetine Dihydrochloride, 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 Dihydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.

S6636New

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.

S7687

GSK269962A HCl

GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

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.

S7935

Y-39983 HCl

Y-39983 is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.

S8448

ZINC00881524 (ROCK inhibitor)

ZINC00881524 is a ROCK inhibitor.

S7936

KD025 (SLx-2119)

KD025 (SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.

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.

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.

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.

Catalog No. 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.

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.

S1573

Fasudil (HA-1077) HCl

Fasudil(HA-1077), 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.

S1474

GSK429286A

GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

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.

S3239New

Emetine Dihydrochloride

Emetine Dihydrochloride, 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 Dihydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.

S6636New

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.

S7687

GSK269962A HCl

GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

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.

S7935

Y-39983 HCl

Y-39983 is a selective rho-associated protein kinase(ROCK) inhibitor with an IC50 of 3.6 nM.

S8448

ZINC00881524 (ROCK inhibitor)

ZINC00881524 is a ROCK inhibitor.

S7936

KD025 (SLx-2119)

KD025 (SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.

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.

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.

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.

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