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.


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ROCK2-IN-6

ROCK2-IN-6 (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research[1].

  • CAS Number: 2260506-59-8
  • MF: C26H21F2N7O
  • MW: 485.49
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Netarsudil mesylate

Netarsudil mesylate is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.

  • CAS Number: 1422144-42-0
  • MF: C30H35N3O9S2
  • MW: 645.744
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RKI-1447

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.

  • CAS Number: 1342278-01-6
  • MF: C16H14N4O2S
  • MW: 326.373
  • Catalog: ROCK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rock-in-d2

ROCK-IN-D2 is an effective and selective inhibitor of ROCK.

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rho Kinase Inhibitor III,Rockout

3-(4-Pyridyl)indole (Rockout) is a Rho-kinase (ROCK) inhibitor, with an IC50 of 25 μM. 3-(4-Pyridyl)indole can inhibit blebbing and cause dissolution of actin stress fibers in a wound healing assay[1].

  • CAS Number: 7272-84-6
  • MF: C13H10N2
  • MW: 194.23200
  • Catalog: ROCK
  • Density: 1.211g/cm3
  • Boiling Point: 406.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 185.2ºC

AR-13503

AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice[1][2].

  • CAS Number: 1254032-16-0
  • MF: C19H19N3O2
  • MW: 321.37
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SAR-407899

SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.

  • CAS Number: 923359-38-0
  • MF: C14H16N2O2
  • MW: 244.289
  • Catalog: ROCK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 517.8±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 267.0±30.1 °C

K-115

Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

  • CAS Number: 887375-67-9
  • MF: C15H23ClFN3O4S
  • MW: 395.877
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rock-in-32

ROCK-IN-32 is an effective Rho-kinase inhibitor.

  • CAS Number: 1013117-40-2
  • MF: C20H17Cl2N3O2
  • MW: 402.28
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thiazovivin

Thiazovivin is a potent ROCK inhibitor, which can protect human embryonic stem cells.

  • CAS Number: 1226056-71-8
  • MF: C15H13N5OS
  • MW: 311.362
  • Catalog: ROCK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rhodblock 6

Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization[1].

  • CAS Number: 886625-06-5
  • MF: C12H13N3O
  • MW: 215.25
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CAY10746

CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR)[1].

  • CAS Number: 2247240-76-0
  • MF: C26H23N3O5
  • MW: 457.478
  • Catalog: ROCK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 664.2±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 355.5±31.5 °C

CMPD101

CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively)[1].

  • CAS Number: 865608-11-3
  • MF: C24H21F3N6O
  • MW: 466.458
  • Catalog: ROCK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Narciclasine

Narciclasine is a plant growth modulator. Narciclasine modulates the Rho/Rho kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity as well as inducing actin stress fiber formation in a RhoA-dependent manner.

  • CAS Number: 29477-83-6
  • MF: C14H13NO7
  • MW: 307.255
  • Catalog: ROCK
  • Density: 1.9±0.1 g/cm3
  • Boiling Point: 733.8±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 397.6±32.9 °C

4-[(1R)-1-Aminoethyl]-N-1H-pyrrolo[2,3-b]pyridin-4-ylbenzamide hydrochloride

Y-33075 hydrochloride (Y-39983) is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.

  • CAS Number: 471843-75-1
  • MF: C16H17ClN4O
  • MW: 316.79
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hu7691

Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].

  • CAS Number: 2360523-76-6
  • MF: C22H22ClF3N4O
  • MW: 450.88
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LX7101

LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.

  • CAS Number: 1192189-69-7
  • MF: C23H29N7O3
  • MW: 451.52100
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Exoenzyme C3, clostridium botulinum

Exoenzyme C3, clostridium botulinum is a promising agent to inactivate RhoA in neurons due to preventing the detrimental effect of active Rho in the recovery of injured neuronal systems. Exoenzyme C3, clostridium botulinum is used for the study of post-traumatic neuro-regeneration[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cotosudil

Cotosudil is a ROCK kinase inhibitor, which can be used for glaucoma or ocular hypertension research[1].

  • CAS Number: 1258833-31-6
  • MF: C16H21N3O2S
  • MW: 319.42
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ROCK2-IN-6 hydrochloride

ROCK2-IN-6 hydrochloride (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research[1].

  • CAS Number: 2762238-94-6
  • MF: C26H22ClF2N7O
  • MW: 521.95
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fasudil Hydrochloride

Fasudil Hydrochloride is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Kis of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

  • CAS Number: 105628-07-7
  • MF: C14H18ClN3O2S
  • MW: 327.83
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: 506.2ºC at 760 mmHg
  • Melting Point: 222 °C(dec.)
  • Flash Point: 259.9ºC

Hydroxy Fasudil Hydrochloride

Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.

  • CAS Number: 155558-32-0
  • MF: C14H18ClN3O3S
  • MW: 343.829
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: >250ºC(dec.)
  • Flash Point: N/A

Sovesudil

Sovesudil, formally known as PHP-201, is a well-tolerated and low toxicity Rho-associated protein kinase (ROCK) inhibitor. Sovesudil can be used for the research of normal-tension glaucoma (NTG)[1].

  • CAS Number: 1333400-14-8
  • MF: C23H22FN3O3
  • MW: 407.438
  • Catalog: ROCK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 545.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 284.0±30.1 °C

Y-27632

Y-27632 is an ATP-competitive inhibitor of ROCK-I and ROCK-II, with Ki of 220 nM and 300 nM for ROCK-I and ROCK-II, respectively.

  • CAS Number: 146986-50-7
  • MF: C14H21N3O
  • MW: 247.34
  • Catalog: ROCK
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 462.6±15.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 233.6±20.4 °C

HA-100 hydrochloride

HA-100 hydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor[1][2].

  • CAS Number: 141543-63-7
  • MF: C13H16ClN3O2S
  • MW: 313.80300
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: 497.4ºC at 760 mmHg
  • Melting Point: 252-254ºC
  • Flash Point: 254.6ºC

GSK429286A

GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.

  • CAS Number: 864082-47-3
  • MF: C21H16F4N4O2
  • MW: 432.371
  • Catalog: ROCK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 688.4±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 370.2±31.5 °C

SB 772077B dihydrochloride

SB-772077B dihydrochloride is an aminofurazan-based Rho kinase( ROCK) inhibitor with IC50s of 5.6 nM and 6 nM toward ROCK1 and ROCK2, respevtively[1].

  • CAS Number: 607373-46-6
  • MF: C15H20Cl2N8O2
  • MW: 415.28
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Scaff10-8

Scaff10-8 is an inhibitor of AKAP-Lbc-RhoA interaction that acts by promoting the translocation of aquaporin-2 to the plasma membrane of renal collecting duct principal cells.

  • CAS Number: 777857-56-4
  • MF: C22H18O6
  • MW: 378.37
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BDP5290

BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.

  • CAS Number: 1817698-21-7
  • MF: C17H18ClN7O
  • MW: 371.82
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HA-100 hydrochloride

HA-100 dihydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 dihydrochloride also used as a ROCK inhibitor[1][2].

  • CAS Number: 210297-47-5
  • MF: C13H17Cl2N3O2S
  • MW: 350.26
  • Catalog: ROCK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A