Rho-Kinases

Rho-kinases (aka Rho-associated coiled-coil kinases or ROCKs) are serine/threonine kinases activated by RhoA GTPases. They are modulators of processes involving cytoskeletal rearrangement such as focal adhesion formation, cell motility and tumor cell invasion.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
4927 AS 1892802
Potent ROCK inhibitor; orally bioavailable
0541 Fasudil hydrochloride
Inhibitor of cyclic nucleotide dependent- and Rho-kinases
4009 GSK 269962
Potent and selective ROCK inhibitor
3726 GSK 429286
Selective Rho-kinase (ROCK) inhibitor
2414 H 1152 dihydrochloride
Selective Rho-kinase (ROCK) inhibitor
2485 Glycyl-H 1152 dihydrochloride
Selective Rho-kinase (ROCK) inhibitor. More selective analog of H 1152 dihydrochloride (Cat. No. 2414)
2415 HA 1100 hydrochloride
Cell-permeable, selective Rho-kinase inhibitor
5182 OXA 06 dihydrochloride
Potent ROCK inhibitor
5061 RKI 1447 dihydrochloride
Potent and selective ROCK inhibitor; antitumor
4118 SB 772077B dihydrochloride
Potent Rho-kinase inhibitor; vasodilator
3667 SR 3677 dihydrochloride
Potent, selective Rho-kinase (ROCK) inhibitor
4961 TC-S 7001
Potent and highly selective ROCK inhibitor; orally active
1254 Y-27632 dihydrochloride
Selective p160ROCK inhibitor

Rho-kinases (aka Rho-associated coiled-coil kinases or ROCKs) are serine/threonine kinases that are activated by RhoA GTPases, and are key modulators of processes involving cytoskeletal rearrangement such focal adhesion formation, cell motility and tumor cell invasion. There are two isoforms of ROCK, ROCKI (aka ROKβ or p160ROCK) and ROCKII (aka ROKα), which share a high degree of structural identity in their kinase domains (92%).

The two Rho-kinase isoforms have different patterns of tissue expression; ROCKII expression is highest in the brain and in muscle whereas ROCKI has a ubiquitous tissue distribution. Subcellularly, ROCKII is found in the cytosol and localizes to the cleavage furrow during cytokinesis. ROCKI is thought to colocalize with the centrosomes. ROCKs phosphorylate a number of proteins involved in actin filament assembly and contraction (e.g. LIM Kinases, MLCK, ERM proteins). Other downstream targets of the Rho kinases include signal transduction molecules such as IRS-1 and PI 3-K/AKT.

External sources of pharmacological information for Rho-Kinases :

    Literature for Rho-Kinases

    Cancer

    Cancer Research Product Guide

    A collection of over 750 products for cancer research, the guide includes research tools for the study of:

    • Cancer Metabolism
    • Epigenetics in Cancer
    • Receptor Signaling
    • Cell Cycle and DNA Damage Repair
    • Angiogenesis
    • Invasion and Metastasis
    Cardiovascular

    Cardiovascular Research Product Guide

    A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

    • Hypertension
    • Thrombosis and Hemostasis
    • Atherosclerosis
    • Myocardial Infarction
    • Ischemia/Reperfusion Injury
    • Arrhythmias
    • Heart Failure
    Kinases

    Kinases Product Listing

    A collection of over 400 products for kinase research, the listing includes inhibitors of:

    • Receptor Tyrosine Kinases
    • Protein Kinases A, C, D and G
    • PI-3 Kinase, Akt and mTOR
    • MAPK Signaling
    • Receptor Serine/Threonine Kinases

    Rho-Kinases Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    ROCKI (ROKβ, p160ROCK) Human ROCK1 NM_005406 Q13464
    Mouse Rock1 NM_009071 P70335
    Rat Rock1 NM_031098 Q63644
    ROCKII (ROKα) Human ROCK2 NM_004850 O75116
    Mouse Rock2 NM_009072 P70336
    Rat Rock2 NM_013022 Q62868