Signaling Pathway

ROCK

ROCK

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ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. ROCKs (ROCK1 and ROCK2) occur in mammals, zebrafish, Xenopus, invertebrates and chicken. Human ROCK1 has a molecular mass of 158 kDa and is a major downstream effector of the small GTPase RhoA. Mammalian ROCK consists of a kinase domain, acoiled-coil region and a Pleckstrin homology (PH) domain, which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular fold if RhoA-GTP is not present. ROCK plays a role in a wide range of different cellular phenomena, as ROCK is a downstream effector protein of the small GTPase Rho, which is one of the major regulators of the cytoskeleton.

ROCK Inhibitors & Modulators (24)

Product Name Catalog No. Brief Description
chroman 1

HY-15392

chroman 1 is a highly potent and selective ROCK II inhibitor.

Fasudil

HY-10341A

Fasudil Hcl(HA-1077; AT-877) 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, respectively.

Fasudil Hydrochloride

HY-10341

Fasudil Hcl(HA-1077; AT-877) 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, respectively.

GSK269962A

HY-15556

GSK269962A(GSK269962) is a potent ROCK inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively); displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.

GSK429286A

HY-11000

GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

H-1152

HY-15720

H-1152, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases.

H-1152 dihydrochloride

HY-15720A

H-1152 2Hcl, an isoquinolinesulfonamide derivative, is a more specific, stronger and membrane-permeable inhibitor of Rho-kinase with a Ki value of 1.6 nM, but poor inhibitor of other serine/threonine kinases.

Hydroxyfasudil

HY-13911

Hydroxyfasudil(HA1100), metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.

Hydroxyfasudil hydrochloride

HY-13911A

Hydroxyfasudil Hcl(HA1100 Hcl), metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.

K-115

HY-15685

K-115, an isoquinolinesulfonamide compound, is a highly selective and potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinical development in patients with POAG or ocular hypertension.

K-115 free base

HY-15685A

K-115, an isoquinolinesulfonamide compound, is a highly selective and potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinical development in patients with POAG or ocular hypertension.

LX7101

HY-12659

LX-7101 is a potent inhibitor of LIMK1/2, ROCK2 and PKA, with IC50 of 24/1.6, 10, and <1 nM.

Narciclasine

HY-16563

Narciclasine is a Rho/Rho kinase/LIM kinase/cofilin signaling pathway activator.

RKI-1447

HY-15755

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2.

ROCK inhibitor

HY-10319

ROCK inhibitor(azaindole 1) is a highly potent inhibitor of human ROCK-1 and ROCK-2 isoenzymes with IC50 values of 0.6 and 1.1 nM, respectively.

SAR407899

HY-15687A

SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.

SAR407899 hydrochloride

HY-15687

SAR407899 Hcl is a potent, ATP-competitive ROCK inhibitor woth Ki value of 36 nM/41 nM for human ROCK/Rat ROCK respectively.

SLx-2119

HY-15307

SLx-2119(KD-025) is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM).

SR-3677

HY-13300

SR-3677 is a new potent and selective ROCK-II inhibitor with an IC50 of ~3 nM in enzyme and cell based assays; IC50 for ROCK-I is 56 ± 12 nM.

Thiazovivin

HY-13257

Thiazovivin (Tzv) is a novel ROCK inhibitor with IC50 of 0.5 μM, promotes hESC survival after single-cell dissociation.