ROCK

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ROCK Inhibitors (8)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
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, 2016, 10.1038/nature17408
  • nature, 2016, 10.1038/nature17408
  • Cell Res, 2013, 23(10):1187-200
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.
  • Cell Res, 2013, 23(10):1187-200
  • Arch Toxicol, 2013, 87(12):2215-31
  • J Mol Cell Cardiol, 2015, 10.1016/j.yjmcc.2015.05.003
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.
  • J Clin Invest, 2014, 124(9):3757-66
  • J Clin Invest, 2014, 124(4):1646-59
  • Diabetes, 2013, 62(5):1697-708
S1474 GSK429286A GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
  • Proc Natl Acad Sci USA, 2014, 111(12):E1140-8
  • Am J Respir Cell Mol Biol, 2014, 50(1):170-9
  • PLoS One, 2014, 9(1):e87281
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.
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) 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.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
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
S7936 KD025 (SLx-2119) <1 mg/mL 90 mg/mL <1 mg/mL
S7995 Ripasudil (K-115) 79 mg/mL 26 mg/mL 5 mg/mL
S7563 AT13148 <1 mg/mL 62 mg/mL <1 mg/mL
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
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