Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008. (xcessbio.com)
GC25482 GSK269962A HCl GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. (glpbio.cn)
GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. (dcchemicals.com)
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2. (dcchemicals.com)
The mainly pathway related to invasion and migration in neoplasic cells is regulated by the Rho GTPases, and their main effectors are the kinases ROCK1 and ROCK2, which are responsible for cytoskeleton control. (fapesp.br)
Inhibitor12
REZUROCK is the first and only FDA-approved small molecule inhibitor of ROCK2, a signaling pathway that modulates inflammatory responses and fibrotic processes. (yahoo.com)
Then, by utilizing varied combinations of diltiazem (voltage-dependent Ca 2+ channel [VDCC] inhibitor), Y27632 (RhoA kinase [ROCK] inhibitor) and chelerythrine (PKC inhibitor) for the effect of DCG on U46619-induced vasoconstriction, we ascertained that DCG inhibits VDCC and ROCK pathway with no effect on PKC. (elsevierpure.com)
Rho-Kinase-IN-1 is a ROCK inhibitor which can be useful for treating diseases or conditions associated with excessive cell proliferation, remodeling, edema and inflammation. (xcessbio.com)
GC66338 ROCK1-IN-1 WAY-624704 is a novel Rho kinases (ROCK) inhibitor with an Ki of 17 nM. (glpbio.cn)
GC38898 CCG-222740 CCG-222740 is a Rho/MRTF pathway inhibitor. (glpbio.cn)
GC36208 H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). (glpbio.cn)
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. (dcchemicals.com)
Hydroxyfasudil Hcl(HA1100 Hcl), metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. (dcchemicals.com)
Chroman 1 dihydrochloride is a highly potent ROCK2 inhibitor, with an IC50 of 1 nM. (dcchemicals.com)
Y-27632 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. (dcchemicals.com)
The Kadmon Corporation's Phase 2 oral drug, KD025, a potent, bio-available and highly selective inhibitor of ROCK2 (Rho-associated coiled-coiled kinase 2) that can be taken orally was designed as one of its priority candidates to treat lupus through the LRxL-STAT Lupus Drug Repositioning Initiative. (lupusnewstoday.com)
We found that TGF-β pre-treatment enhanced acute contractile responses to bradykinin (BK) in isolated rat bronchioles, and inhibitors of RhoGEFs (Y16) and Rho-kinase (Y27632), but not the SrcFK inhibitor PP2 prevented this enhancement. (kcl.ac.uk)
Serine-threoni1
Rho-associated protein kinase (ROCK) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine specific protein kinases. (wikipedia.org)
RhoA8
Mammalian ROCK consists of a kinase domain, a coiled-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. (wikipedia.org)
In VSMCs, long-term treatment with DCG had no effect on ROCK2 and RhoA expression. (elsevierpure.com)
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. (dcchemicals.com)
Transforming growth factor-β (TGF-β), RhoA/Rho-kinase and Src-family kinases (SrcFK) have independently been implicated in airway hyper-responsiveness, but how they interact in order to regulate airway smooth muscle contractility is not fully understood. (kcl.ac.uk)
In cultured human airway smooth muscle cells (hASMC), TGF-β pre-treatment enhanced the protein expression of the Rho guanine nucleotide exchange factor ARHGEF1, MLC20, MYPT-1 and the actin-severing protein cofilin, but not of RhoA, ROCK2 or c-Src. (kcl.ac.uk)
Our data indicate that TGF-β enhances BK-induced contraction, RhoA translocation and Rho-kinase activity in airway smooth muscle largely via ARHGEF1, but independently of SrcFK and total RhoA-GTP content. (kcl.ac.uk)
Ключевым активатором Rho-киназы является малый гуанозинтрифосфат (ГТФ)-связывающий белок RhoA, но существуют и RhoA-независимые механизмы регуляции этого фермента. (almazovcentre.ru)
7. Shimokawa H, Sunamura S, Satoh K. RhoA/Rho-Kinase in the cardiovascular system. (almazovcentre.ru)
Contraction4
these calcium ions, in turn stimulate a myosin light chain kinase, forcing a contraction. (wikipedia.org)
3. Nishimura J, Bi D, Kanaide H. Dependence of proliferating dedifferentiated vascular smooth muscle contraction on Rho-Rho kinase system. (almazovcentre.ru)
Selective1
Selective inhibition of brain endothelial Rho-kinase- 2 provides optimal protection of an in vitro blood-brain barrier from tissue-type plasminogen activator and plasmin. (pai-2.com)
Cytoskeleton4
Rho-associated kinase (ROCK), including the ROCK-I and ROCK-II isoforms, is a protein kinase involved in signaling from Rho to actin cytoskeleton. (antibodyguide.com)
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. (wikipedia.org)
Rho GTPases act as molecular switches to regulate the actin cytoskeleton for cytokinesis, of which Rac1 is regulated by MgcRacGAP. (shengsci.com)
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC family of serine-threonine kinases and takes part in regulating the shape and movement of cells by acting on the cytoskeleton. (glpbio.cn)
Formation of actin stress fibers1
Thus in both cases, ROCK activation by Rho induces the formation of actin stress fibers, actin filament bundles of opposing polarity, containing myosin II, tropomyosin, caldesmon and MLC-kinase, and consequently of focal contacts, which are immature integrin-based adhesion points with the extracellular substrate. (wikipedia.org)
Inhibitors1
Furthermore, the present invention relates to the use of said disubstituted pyridine derivatives as inhibitors for a protein kinase. (justia.com)
Isoforms1
Studies also revealed a previously undescribed shift in ROCK isoforms in lymphatic endothelial cells, wherein a ROCK2/junctional adhesion molecule-A (JAM-A) complex emerges that is responsible for the cytokine-induced lymphatic junction zippering. (lymphoedemaeducation.com.au)
Phosphatase5
1. ROCK is a key regulator of actin organization and thus a regulator of cell migration as follows: Different substrates can be phosphorylated by ROCKs, including LIM kinase, myosin light chain (MLC) and MLC phosphatase. (wikipedia.org)
Mitogen-activated protein kinase phosphatases (MKPs) belongs to the dual-specificity phosphatase (DUSP) family. (cancer-research-network.com)
Many molecular pathways in eukaryotic cells are modulated by specific signaling proteins that are controlled, by phosphorylation and dephosphorylation, through the activity of kinase and phosphatase enzymes. (biomedcentral.com)
This interaction activates AltR/LILRB3, which triggers an intracellular pathway called SHP2-ROCK2 (Src homology-2 domain-containing protein tyrosine phosphatase-2-Rho-associated protein kinase 2). (asiabiotech.com)
6. Somlyo AP, Somlyo AV. Ca2+ sensitivity of smooth muscle and nonmuscle myosin II: modulated by G proteins, kinases, and myosin phosphatase. (almazovcentre.ru)
Myosin1
Rat ROCKs were discovered as the first effectors of Rho and they induce the formation of stress fibers and focal adhesions by phosphorylating MLC (myosin light chain). (wikipedia.org)
Receptor2
KEGG pathways enrichment and PPI network indicate four major pathways, including extracellular matrix -receptor interaction, focal adhesion, phosphatidylinositol 3-kinase (PI3K)-Protein kinase B (Akt), and Ras signaling pathways were involved in the degeneration of cartilage. (nature.com)
Y-27632 inhibited the kinase activity of both ROCK-I and ROCK-II in vitro, and this inhibition was reversed by ATP in a competitive manner. (bioquote.com)
This opposing response was further demonstrated when inhibition of rho-associated protein kinase (ROCK) was found to normalize fluid drainage under cytokine challenge by simultaneously loosening lymphatic junctions and tightening blood vessel junctions. (lymphoedemaeducation.com.au)
Rho-kinase (ROCK) inhibition, widely used in cardiovascular disease, could protect the blood-brain barrier (BBB) from damage during thrombolysis rt-PA-induced. (pai-2.com)
Vitro1
To validate these in vitro findings, we further demonstrated in a genetic mouse model that lymphatic-specific knockout of ROCK2 reversed lymphedema in vivo. (lymphoedemaeducation.com.au)
Threonine4
Serine/threonine kinase ROCK II/Rho kinase,which is an isozyme of ROCK I, is one of the targets for the small GTPase Rho. (antibodyguide.com)
Rho-associated protein kinase are serine or threonine kinases that determine the calcium sensitivity in smooth muscle cells. (wikipedia.org)
DUSP-MKPs dephosphorylate and inactivate the MAPKs extracellular signal-regulated kinase (ERK), JNK/SAPK, and p38 on tyrosine and threonine residues. (cancer-research-network.com)
displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. (dcchemicals.com)
ELISA2
Description: A competitive ELISA for quantitative measurement of Rat S phase kinase associated protein 1(SKP1) in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. (unicoupi.com)
Description: A sandwich ELISA kit for detection of Protein Kinase C Alpha from Human in samples from blood, serum, plasma, cell culture fluid and other biological fluids. (scalegen.com)
Vascular1
4. Shimizu T, Fukumoto Y, Tanaka SI, Satoh K, Ikeda S, Shimokawa H. Crucial role of ROCK2 in vascular smooth muscle cells for hypoxia-induced pulmonary hypertension in mice. (almazovcentre.ru)
Compound1
At the International Centre for Kinase Profiling (ICKP) we understand that ascertaining how your compound behaves in relation to the multitude of related enzymes is critical. (mrc.ac.uk)
These substrates, once phosphorylated, regulate actin filament organization and contractility as follows: Amount of actin filaments ROCK inhibits the depolymerization of actin filaments indirectly: ROCK phosphorylates and activates LIM kinase, which in turn phosphorylates ADF/cofilin, thereby inactivating its actin-depolymerization activity. (wikipedia.org)
Recombinant1
Immunogen Partial recombinant corresponding to aa1279-1388 from ROCK2 (NP_004841) with GST tag. (antibodyguide.com)
Inflammatory1
Method for the treatment and prevention of the inflammatory diseases using Rho kinase inhibiting compounds. (xcessbio.com)
Activity2
The pro-apoptotic protease, caspase 3, activates ROCK kinase activity by cleaving the C-terminal PH domain. (wikipedia.org)
ROCK2) have the potential to be developed into semomorphic drugs as they change SASP composition and reduce senescence cell secretory activity. (phiab.com)
Genetic1
At the University of California, San Diego (UCSD) and the VA San Diego Healthcare System, hypertension researchers have focused on exploring the role of Rho/Rho kinase (ROCK) genetic variations in blood pressure (BP) regulation by probing heritability in human twins. (dynapulse.com)
Human2
Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Protein Kinase C Alpha (PKCa) in serum, plasma, tissue homogenates and other biological fluids. (scalegen.com)
Description: Enzyme-linked immunosorbent assay based on the Double-antibody Sandwich method for detection of Human Protein Kinase C Alpha (PKCa) in samples from serum, plasma, tissue homogenates and other biological fluids with no significant corss-reactivity with analogues from other species. (scalegen.com)
Hypertension1
DynaPulse 5200A/Pathway and DAC used for monitoring hemodynamics in ROCK2 study Hypertension 2006;47:1-11, by TM Seasholtz, DT O Connor, et.al. (dynapulse.com)
Previously1
These studies provide a unique platform to generate interstitial fluid pressure and measure the drainage of interstitial fluid into lymphatics and reveal a previously unappreciated ROCK2-mediated mechanism in regulating lymphatic drainage. (lymphoedemaeducation.com.au)
Brain1
However, ROCK2 is distributed mostly in the brain and heart. (wikipedia.org)
Cell1
In this work, Y. D. Simay with colleagues evaluated if Rho/Rho kinase pathway could be a target for potential drugs in doxorubicin-induced senescent cancer cell lines. (phiab.com)