ROCK

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1049 Y-27632 2HCl 14 mg/mL 64 mg/mL <1 mg/mL
S1459 Thiazovivin <1 mg/mL 15 mg/mL <1 mg/mL
S1573 Fasudil (HA-1077) HCl 65 mg/mL 5 mg/mL <1 mg/mL
S1474 GSK429286A <1 mg/mL 87 mg/mL 4 mg/mL
S7195 RKI-1447 <1 mg/mL 65 mg/mL <1 mg/mL
S8489 GSK180736A (GSK180736) <1 mg/mL 73 mg/mL 3 mg/mL
S8208 Hydroxyfasudil (HA-1100) HCl 60 mg/mL 68 mg/mL <1 mg/mL
S8448 ZINC00881524 (ROCK inhibitor) <1 mg/mL 76 mg/mL 3 mg/mL
S7935 Y-39983 HCl 63 mg/mL 63 mg/mL 2 mg/mL
S8226 Netarsudil (AR-13324) 2HCl 54 mg/mL 20 mg/mL 2 mg/mL
S7687 GSK269962 HCl <1 mg/mL 100 mg/mL 6 mg/mL
S7936 KD025 (SLx-2119) <1 mg/mL 90 mg/mL <1 mg/mL
S7995 Ripasudil (K-115) hydrochloride dihydrate 79 mg/mL 26 mg/mL 5 mg/mL
S7563 AT13148 <1 mg/mL 62 mg/mL <1 mg/mL

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), 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.

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.

S8489New

GSK180736A (GSK180736)

GSK180736A, developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.

S8208New

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.

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) 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.

S7687New

GSK269962 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.

S7936

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.

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.

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