ROCK

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

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) HCl is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM in cell-free assays, respectively.

S1474

GSK429286A

GSK429286A 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.

S8448New

ZINC00881524 (ROCK inhibitor)

ZINC00881524 is a ROCK inhibitor.

S7935New

Y-39983 HCl

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

S8226New

Netarsudil (AR-13324)

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.

S7687New

GSK269962

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

S7936New

KD025 (SLx-2119)

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

S7995New

Ripasudil (K-115)

Ripasudil (K-115) 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.

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) HCl is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM in cell-free assays, respectively.

S1474

GSK429286A

GSK429286A 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.

S8448New

ZINC00881524 (ROCK inhibitor)

ZINC00881524 is a ROCK inhibitor.

S7935New

Y-39983 HCl

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

S8226New

Netarsudil (AR-13324)

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.

S7687New

GSK269962

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

S7936New

KD025 (SLx-2119)

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

S7995New

Ripasudil (K-115)

Ripasudil (K-115) 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.

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