Replaces Prod. #: BML-EI299
- Selective inhibitor of ROCK1 and ROC/2
- Highly potent inhibitor of smooth muscle contractions
- Media component used in the cryopreservation of stem cells
- Applications in cancer, cardiology, nephrology, neurology, and stem cell studies
- Highly cited
Y-27632 is a highly potent, cell permeable, selective and ATP competitive inhibitor of ROCK1 and ROCK2 (IC50=800nM). It acts as a potent inhibitor of agonist-induced Ca2+sensitization of myosin phosphorylation and smooth muscle contractions, blocks cell spreading, and suppresses RhoA-induced formation of stress fibers in hepatic stellate cells. Y-27632 significantly reduces the increase of inflammatory cytokines after reperfusion, preventing the development of acute renal failure. There are numerous application for this compound including: anti-nociceptive effect, cardioprotective effects, inhibition of superoxide production, mimicking effect of β-agonists on human cells, and suppression of tumor cell invasion.
There has been a growing interest in Y-27632 for use in stem cell self-renewal and reprogramming. It is known to increase the survival rate of human embryonic stem cells undergoing cryopreservation.
Product Details
| Alternative Name: | (R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide . 2HCl |
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| Formula: | C14H21N3O . 2HCl |
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| MW: | 247.3 . 73.0 |
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| CAS: | 129830-38-2 |
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| Purity: | ≥98% (HPLC (UV)) |
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| Purity Detail: | Enantiomeric excess ≥96% |
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| Identity: | Identity determined by MS and NMR. |
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| Appearance: | White to pale yellow powder. |
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| Solubility: | Soluble in DMSO (25mg/ml), methanol (25mg/ml), acetonitrile (<1mg/ml), dioxane (<1mg/ml), water (very soluble). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Stock solutions are stable for up to 1 month when stored at -20°C. |
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| Handling: | Protect from light. Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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The interaction of β-arrestin1 with talin1 driven by endothelin A receptor as a feature of α5β1 integrin activation in high-grade serous ovarian cancer: I. Masi, et al.; Cell Death Dis.
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Primary cilia and SHH signaling impairments in human and mouse models of Parkinson’s disease: W. Wurst, et al.; Nat. Commun.
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Response of TGF-β isoforms in epithelial-mesenchymal transition of enamel epithelial cells: Y. Miyakawa, et al.; Arch. Oral. Biol.
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Transcriptome reprogramming of Epstein-Barr virus infected epithelial and B cells reveals distinct host-virus interaction profiles: N. Ma, et al.; Cell Death Dis.
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Treating intrauterine adhesion using conditionally reprogrammed physiological endometrial epithelial cells: S. Xia, et al.; Stem Cell Res. Ther.
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Biomechanical Strain Promotes the Differentiation of Murine Oogonial Stem Cells: J.A. MacDonald, et al.; Stem Cells Dev.
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Deciphering cell signaling networks with massively multiplexed biosensor barcoding: J-M. Yang, et al.; Cell
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Defective metabolic programming impairs early neuronal morphogenesis in neural cultures and an organoid model of Leigh syndrome: G. Inak, et al.; Nat. Commun.
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Directed differentiation of human pluripotent stem cells into epidermal stem and progenitor cells: S. Ruiz-Torres, et al.; Mol. Biol. Rep.
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Epigenetic modulation of immune synaptic-cytoskeletal networks potentiates γδ T cell-mediated cytotoxicity in lung cancer: R.R. Weng, et al.; Nat. Commun.
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Epithelial miR-141 regulates IL-13-induced airway mucus production: S. Siddiqui, et al.; JCI Insight
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Establishment of porcine and monkey colonic organoids for drug toxicity study: H. Li, et al.; Cell Regen.
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Functional diagnostics using fresh uncultured lung tumor cells to guide personalized treatments: S.S. Talwelkar, et al.; Cell Rep. Med.
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Generation of human iPSC-derived neural progenitor cells (NPCs) as drug discovery model for neurological and mitochondrial disorders: A. Zink, et al.; Bio. Protoc.
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H3. 3-K27M drives neural stem cell-specific gliomagenesis in a human iPSC-derived model: D. Haag, et al.; Cancer Cell
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Identification and characterization of a novel Epstein-Barr Virus-encoded circular RNA from LMP-2 Gene: K. E. Tan, et al.; Sci. Rep.
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Inherited DNA repair defects disrupt the structure and function of human skin: S. Ruiz-Torres, et al.; Cell Stem Cell
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LFA-1 and Kindlin-3 enable the collaborative transport of SLP-76 microclusters by myosin and dynein motors: K.P. Eidell, et al.; J. Cell Sci.
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Long-Term Maintenance of Viable Adult Rat Sertoli Cells Able to Establish Testis Barrier Components and Function in Response to Androgens: H. Kabbesh, et al.; Cells
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Mouse papillomavirus type 1 (MmuPV1) DNA is frequently integrated in benign tumors by microhomology-mediated end-joining: L. Yu, et al.; PLoS Pathog.
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Non-invasive and high-throughput interrogation of exon-specific isoform expression: D.J.J. Truong, et al.; Nat. Cell Biol.
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Patient-derived organotypic epithelial rafts model phenotypes in juvenile-onset recurrent respiratory papillomatosis: M.C. Bedard, et al.; Viruses
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Probing TGF-β1-induced cytoskeletal rearrangement by fluorescent-labeled silica nanoparticle uptake assay: H.R. Shin, et al.; Biochem. Biophys. Rep.
28, 101137 (2021),
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Profiling of conditionally reprogrammed cell lines for in vitro chemotherapy response prediction of pancreatic cancer: H.S. Lee, et al.; EBioMedicine
65, 103218 (2021),
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10, 2622 (2021),
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RAB19 directs cortical remodeling and membrane growth for primary ciliogenesis: C.E. Jewett, et al.; Dev. Cell
56, 325 (2021),
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Reprogramming of two induced pluripotent stem cell lines from a heterozygous GRIN2D developmental and epileptic encephalopathy (DEE) patient (BGUi011-A) and from a healthy family relative (BGUi012-A): T. Rabinski, et al.; Stem Cell Res.
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Reuse of Cell Culture Inserts for in vitro Human Primary Airway Epithelial Cell Studies: T. Kato, et al.; Am. J. Respir. Cell Mol. Biol.
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Sex-Specific Isolation and Propagation of Human Premeiotic Fetal Germ Cells and Germ Cell-Like Cells: S. Mishra, et al.; Cells
10, 1214 (2021),
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Simplification of culture conditions and feeder-free expansion of bovine embryonic stem cells: D.A. Soto, et al.; Sci. Rep.
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Surfactant protein C mutation links postnatal type 2 cell dysfunction to adult disease: S. Sitaraman, et al.; JCI Insight
6, e142501 (2021),
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6, 35 (2020),
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A rapid quantification of invasive phenotype in head and neck squamous cell carcinoma: A novel 3D pillar array system: S. Y. Choi, et al.; Oral Oncol.
108, 104807 (2020),
Application(s): Increase the viability of primary cancer cells.,
Abstract;
A variant of SLC1A5 is a mitochondrial glutamine transporter for metabolic reprogramming in cancer cells: H.C. Yoo, et al.; Cell Metab.
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An excitable Ras/PI3K/ERK signaling network controls migration and oncogenic transformation in epithelial cells: H. Zhan, et al.; Dev. Cell.
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Assessment of ethanol-induced toxicity on IPSC-derived human neurons using a novel high-throughput mitochondrial neuronal health (MNH) assay: A. Zink, et al.; Front. Cell. Dev. Biol.
8, 590540 (2020),
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Chromatin remodeling in bovine embryos indicates species-specific regulation of genome activation: M.M. Halstead, et al.; Nat. Commun.
11, 4654 (2020),
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Destabilization of β-catenin and RAS by Targeting the Wnt/β-catenin Pathway as a Potential Treatment for Triple-Negative Breast Cancer: W. Ryu, et al.; Exp. Mol. Med.
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Efficient propagation of circulating tumor cells: a first step for probing tumor metastasis: J. Xiao, et al.; Cancers
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Forces during cellular uptake of viruses and nanoparticles at the ventral side: T. Wiegand, et al.; Nat. Commun.
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Human bocavirus 1 infection of well‐differentiated human airway epithelium: Z. Yan, et al.; Curr. Protoc. Microbiol.
58, e107 (2020),
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Murine neuroblastoma cell lines developed by conditional reprogramming preserve heterogeneous phenotypes observed in vivo: E. Krawczyk, et al.; Lab. Invest.
100, 38 (2020),
Application(s): Culture and cryopreservation medium for neuroblastoma cell cultures,
Abstract;
Full Text
Nanosecond pulsed current under plasma-producing conditions induces morphological alterations and stress fiber formation in human fibrosarcoma HT-1080 cells: C.H. Chang, et al.; Arch. Biochem. Biophys.
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SARS-CoV-2 reverse genetics reveals a variable infection gradient in the respiratory tract: Y.J. Hou, et al.; Cell
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The anti-tumor function of the IKK inhibitor PS1145 and high levels of p65 and KLF4 are associated with the drug resistance in nasopharyngeal carcinoma cells: H.L. Lung, et al.; Sci. Rep.
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18, 5097 (2019),
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25, 93 (2019),
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Characterization of primary human mammary epithelial cells isolated and propagated by conditional reprogrammed cell culture: L. Jin, et al.; Oncotarget
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2018, ERC-17-0447 (2018),
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Generation of renewable mouse intestinal epithelial cell monolayers and organoids for functional analyses: E.C. Moorefield, et al.; BMC Cell Biol.
19, 15 (2018),
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Long-term expansion of primary equine keratinocytes that maintain the ability to differentiate into stratified epidermis: F. Alkhilaiwi, et al.; Stem Cell Res. Ther.
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Long-Term In Vitro Expansion of Epithelial Stem Cells Enabled by Pharmacological Inhibition of PAK1-ROCK-Myosin II and TGF-β Signaling: C. Zhang, et al.; Cell Rep.
3, 598 (2018),
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14, 10 (2018),
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WNT9A Is a Conserved Regulator of Hematopoietic Stem and Progenitor Cell Development: J. Richter, et al.; Genes
9, 66 (2018),
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xCT (SLC7A11)-mediated metabolic reprogramming promotes non-small cell lung cancer progression: X. Ji, et al.; Oncogene
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A genome-wide screen identifies YAP/WBP2 interplay conferring growth advantage on human epidermal stem cells: G. Walko, et al.; Nat. Commun.
8, 14744 (2017),
Abstract;
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Conditionally reprogrammed normal and primary tumor prostate epithelial cells: a novel patient-derived cell model for studies of human prostate cancer: O.A. Timofeeva, et al.; Oncotarget
8, 22741 (2017),
Application(s): Cell culture,
Abstract;
Full Text
Epithelial tension in the second heart field promotes mouse heart tube elongation: A. Francou, et al.; Nat. Commun.
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Functional Transcriptomics in Diverse Intestinal Epithelial Cell Types Reveals Robust MicroRNA Sensitivity in Intestinal Stem Cells to Microbial Status: B.C. Peck, et al.; J. Biol. Chem.
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Human iPSC-Derived Neural Progenitors Are an Effective Drug Discovery Model for Neurological mtDNA Disorders: C. Lorenz, et al.; Cell Stem Cell
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Loss of Tpm4.1 leads to disruption of cell-cell adhesions and invasive behavior in breast epithelial cells via increased Rac1 signaling: S. Jeong, et al.; Oncotarget
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Potential antitumor activity and apoptosis induction of Glossostemon bruguieri root extract against hepatocellular carcinoma cells: M.S. Alwhibi, et al.; Evid. Based Complement Alternat. Med.
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Application(s): Cell culture,
Abstract;
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The full transcription map of mouse papillomavirus type 1 (MmuPV1) in mouse wart tissues: X.Y. Xue, et al.; PLoS Pathog.
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TOP2A and EZH2 provide early detection of an aggressive prostate cancer subgroup: D.P. Labbé, et al.; Clin. Cancer Res.
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Tropomyosin isoform Tpm2.1 regulates collective and amoeboid cell migration and cell aggregation in breast epithelial cells: H. Shin, et al.; Oncotarget
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A comparison of strategies for immortalizing mouse embryonic fibroblasts: M.M. St. Amad, et al.; J. Biol. Methods
3, e41 (2016),
Application(s): Immortalization via Rock inhibitor supplementation,
Full Text
Caffeine Suppresses the Progression of Human Glioblastoma via Cathepsin B and MAPK Signaling Pathway: Y.C. Cheng, et al.; J. Nutr. Biochem.
33, 63 (2016),
Application(s): Cell culture,
Abstract;
Down-regulation of 14-3-3 Zeta Inhibits TGF-β1-Induced Actomyosin Contraction in Human Trabecular Meshwork Cells Through RhoA Signaling Pathway: Y. Ye, et al.; Invest. Ophthalmol. Vis. Sci.
57, 719 (2016),
Application(s): Cell culture,
Abstract;
Full Text
Endothelin A receptor drives invadopodia function and cell motility through the β-arrestin/PDZ-RhoGEF pathway in ovarian carcinoma: E. Semprucci, et al.; Oncogene
35, 3432 (2016),
Application(s): Cell culture ,
Abstract;
Generation and characterization of rat liver stem cell lines and their engraftment in a rat model of liver failure: E.W. Kuijk, et al.; Sci. Rep.
6, 22154 (2016),
Application(s): Rat liver stem cell isolation and culture,
Abstract;
Full Text
Generation of a C57BL/6 MYC-Driven Mouse Model and Cell Line of Prostate Cancer: L. Ellis, et al.; Prostate
13, 1192 (2016),
Abstract;
Full Text
Single-cell functional analysis of parathyroid adenomas reveals distinct classes of calcium sensing behaviour in primary hyperparathyroidism: J. Koh, et al. ; J. Cell Mol. Med.
20, 351 (2016),
Application(s): Cell culture,
Abstract;
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Single‐cell functional analysis of parathyroid adenomas reveals distinct classes of calcium sensing behaviour in primary hyperparathyroidism: J. Koh, et al.; J. Cell. Mol. Med.
2, 351 (2016),
Abstract;
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The impact of low-frequency, low-force cyclic stretching of human bronchi on airway responsiveness: M. Le Guen, et al.; Respir. Res.
17, 151 (2016),
Abstract;
Full Text
Generation of iPSCs as a Pooled Culture Using Magnetic Activated Cell Sorting of Newly Reprogrammed Cells: W. Yang, et al.; PLoS One
10, e0134995 (2015),
Application(s): Cell culture,
Abstract;
Full Text
High-efficiency reprogramming of fibroblasts into cardiomyocytes requires suppression of pro-fibrotic signalling: Y. Zhao, et al.; Nat. Commun.
6, 8243 (2015),
Application(s): Cell Culture,
Abstract;
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The effect of ROCK on TNF-α-induced CXCL8 secretion by intestinal epithelial cell lines is mediated through MKK4 and JNK signaling: A.C. Perey, et al.; Cell Immunol.
293, 80 (2015),
Application(s): Cell Culture,
Abstract;
Vaginal innate immune mediators are modulated by a water extract of Houttuynia cordata Thunb: S. Satthakarn, et al.; BMC Complement. Altern. Med.
15, 183 (2015),
Application(s): Cell Culture,
Abstract;
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Strigolactone analogues induce apoptosis through activation of p38 and the stress response pathway in cancer cell lines and in conditionally reprogrammed primary prostate cancer cells: C.B. Pollock, et al.; Oncotarget
5, 1683 (2014),
Application(s): Cell Culture,
Abstract;
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Dissecting the roles of ROCK isoforms in stress-induced cell detachment
: J. Shi, et al. ; Cell Cycle
12, 1492 (2013),
Abstract;
Distinct roles for ROCK1 and ROCK2 in the regulation of cell detachment: J. Shi, et al.; Cell Death Dis.
4, e483 (2013),
Abstract;
Full Text
Conditionally reprogrammed cells represent a stem-like state of adult epithelial cells: F.A. Suprynowicz, et al. ; PNAS
109, 20035 (2012),
Abstract;
ROCK Inhibitor and Feeder Cells Induce the Conditional Reprogramming of Epithelial Cells : X. Liu, et al.; Am. J. Pathol.
180, 599,607 (2012),
Abstract;
Use of reprogrammed cells to identify therapy for respiratory papillomatosis: H. Yuan, et al. ; N. Engl. J. Med.
367, 1220 (2012),
Abstract;
Small molecule inhibition of cytoskeletal dynamics in melanoma tumors results in altered transcriptional expression patterns of key genes involved in tumor initiation and progression: C. Spencer, et al.; Cancer Genom. Proteom.
8, 77 (2011),
Abstract;
Effects of rho-kinase inhibition on pulmonary hypertension, lung growth, and structure in neonatal rats chronically exposed to hypoxia: AJ. Ziino, et al.; Pediatr. Res.
67, 177 (2010),
Abstract;
The proline-rich region of HIV-1 Nef affects CXCR4-mediated chemotaxis in Jurkat T cells: C.M. Lee, et al.; Viral Immunol.
21, 347 (2008),
Abstract;
Molecular characterization of the effects of Y-27632: H. Darenfed, et al.; Cell Motil. Cytoskeleton
64, 97 (2007),
Abstract;
A Rho-kinase inhibitor, Y-27632, reduces cholinergic contraction but not neurotransmitter release: L. Fernandes, et al.; Eur. J. Pharmacol.
550, 155 (2006),
Abstract;
Rho-kinase inhibitor, Y-27632, has an antinociceptive effect in mice: K. Buyukafsar, et al.; Eur. J. Pharmacol.
541, 49 (2006),
Abstract;
Structural basis for induced-fit binding of Rho-kinase to the inhibitor Y-27632: H. Yamaguchi, et al.; J. Biochem.
140, 305 (2006),
Abstract;
Preventive effect of Y-27632, a selective Rho-kinase inhibitor, on ischemia/reperfusion-induced acute renal failure in rats: K. Teraishi, et al.; Eur. J. Pharmacol.
505, 205 (2004),
Abstract;
Comparison of effects of Y-27632 and Isoproterenol on release of cytokines from human peripheral T cells: M. Aihara, et al.; Int. Immunopharmacol.
3, 1619 (2003),
Abstract;
Inhibition of high K+-induced contraction by the ROCKs inhibitor Y-27632 in vascular smooth muscle: possible involvement of ROCKs in a signal transduction pathway: K. Sakamoto, et al.; J. Pharmacol. Sci.
92, 56 (2003),
Abstract;
Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity: C. Breitenlechner, et al.; Structure
11, 1595 (2003),
Abstract;
Y-27632, a Rho-kinase inhibitor, inhibits proliferation and adrenergic contraction of prostatic smooth muscle cells: R.W. Rees, et al.; J. Urol.
170, 2517 (2003),
Abstract;
Antagonism of Rho-kinase stimulates rat penile erection via a nitric oxide-independent pathway: K. Chitaley, et al.; Nat. Med.
7, 119 (2001),
Abstract;
Inhibition of intrahepatic metastasis of human hepatocellular carcinoma by Rho-associated protein kinase inhibitor Y-27632: M. Takamura, et al.; Hepatology
33, 577 (2001),
Abstract;
A p160ROCK-specific inhibitor, Y-27632, attenuates rat hepatic stellate cell growth: H. Iwamoto, et al.; J. Hepatol.
32, 762 (2000),
Abstract;
Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases: T. Ishizaki, et al.; Mol. Pharmacol.
57, 976 (2000),
Abstract;
Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J.
351, 95 (2000),
Abstract;
Full Text
The effect of a Rho kinase inhibitor Y-27632 on superoxide production, aggregation and adhesion in human polymorphonuclear leukocytes: A. Kawaguchi, et al.; Eur. J. Pharmacol.
403, 203 (2000),
Abstract;
Use and properties of ROCK-specific inhibitor Y-27632: S. Narumiya, et al.; Meth. Enzymol.
325, 273 (2000),
Abstract;
Y-27632, an inhibitor of rho-associated protein kinase, suppresses tumor cell invasion via regulation of focal adhesion and focal adhesion kinase: F. Imamura, et al.; Jpn. J. Cancer Res.
91, 811 (2000),
Abstract;
Signaling from Rho to the actin cytoskeleton through protein kinases ROCK and LIM-kinase: M. Maekawa, et al.; Science
285, 895 (1999),
Abstract;
Molecular dissection of the Rho-associated protein kinase (p160ROCK)-regulated neurite remodeling in neuroblastoma N1E-115 cells: M. Hirose, et al.; J. Cell Biol.
141, 1625 (1998),
Abstract;
Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension: M. Uehata, et al.; Nature
389, 990 (1997),
Abstract;
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