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Rho Activator II

Rho Activator II
$0.00
SKU
CN03
Datasheet
MSDS
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Product Uses Include

  • Activator for Rho pathway
  • Study the effects of Rho activation on cell motility
  • Study the effects of Rho activation on the rearrangement of the actin cytoskeleton
  • Investigate the effects of Rho activation with respect to cross talk with other signal transduction pathways
      Click Here for Detailed Methods
      G-Switch-Logo-_White-BG_


      The G-switch™ Direct Modulators have been developed with an emphasis on creating highly potent cell permeable reagents that directly target the Rho family of small G-proteins.  Our Direct Activator reagents are based on the catalytic domain of the bacterial CNF toxins, which are covalently attached to a proprietary cell penetrating moiety.  Rho Activator II (Cat# CN03) enters the cell and activates Rho GTPase isoforms by deamidating glutamine-63, which is located in the Switch II region of these GTPases (1).  This modification converts glutamine-63 to glutamate, which blocks intrinsic and GAP stimulated GTPase activity resulting in constitutively active Rho (2).  Rho Activator II robustly increases the level of GTP bound RhoA within 2-4 h after addition to the culture medium, providing a more rapid alternative to transfection based methods for introducing activators like GEFs into cells.  Moreover, the targeted action of Rho Activator II makes it far more attractive tool for the study of Rho GTPase signaling than classic indirect activators (e.g. LPA) that concomitantly activate other signaling pathways (e.g. Ras, PI3K and PLC).

       

      References

      • Schmidt, G., et al., Gln 63 of Rho is deamidated by Escherichia coli cytotoxic necrotizing factor-1. Nature, 1997. 387(6634): p. 725-9.
      • Flatau, G., et al., Toxin-induced activation of the G protein p21 Rho by deamidation of glutamine. Nature, 1997. 387(6634): p. 729-33.

      For product Datasheets and MSDSs please click on the PDF links below.   For additional information, click on the FAQs tab above or contact our Technical Support department at tservice@cytoskeleton.com

      AuthorTitleJournalYearArticle Link
      Tran, Sydnie K. et al.P-cadherin-dependent adhesions are required for single lumen formation and HGF-mediated cell protrusions during epithelial morphogenesisiScience2025
      Aviram, Rohtem et al.Coordination among cytoskeletal organization, cell contraction, and extracellular matrix development is dependent on LOX for aneurysm preventionThe FEBS Journal2025
      Frey, Kerstin et al.Curvature Perception of Mesenchymal Cells on Mesoscale TopographiesAdvanced Healthcare Materials2025
      Saleem, Hafiza Nosheen et al.3D Computational Modeling of Defective Early Endosome Distribution in Human iPSC-Based Cardiomyopathy ModelsCells2024
      Wang, Ting Ching et al.Genetic variation drives cancer cell adaptation to ECM stiffnessProceedings of the National Academy of Sciences2024
      Jipp, Marcel et al.Cell-substrate distance fluctuations of confluent cells enable fast and coherent collective migrationCell Reports2024
      Pho, Mai et al.Actin contraction controls nuclear blebbing and rupture independent of actin confinementMolecular biology of the cell2024
      Venugopal, Shruthi et al.Regulation of the RhoA exchange factor GEF-H1 by pro-fibrotic stimuli through a positive feedback loop involving RhoA, MRTF and Sp1American Journal of Physiology-Cell Physiology2024
      Tokic, Silvija et al.The RhoA guanine exchange factor ABR: a glucose-sensitive mediator of actin reorganization in feto-placental arterial endothelial cells altered by gestational diabetes mellitusThe Journal of Physiology2024
      Burch, A P ; et al.Reduction of N-Acetylglucosaminyltransferase-I Activity Promotes Neuroblastoma Invasiveness and EGF-Stimulated Proliferation In VitroInternational Journal of Translational Medicine2024
      Weiß, Martin S. et al.Matrix Resistance Toward Proteolytic Cleavage Controls Contractility-Dependent Migration Modes During Angiogenic SproutingAdvanced Science2024
      Ren, Xiaoyu et al.Loss of Myo19 increases metastasis by enhancing microenvironmental ROS gradient and chemotaxisEMBO Reports2024
      Zhang, Chunlei et al.mTORC1 Mediates Biphasic Mechano-Response to Orchestrate Adhesion-Dependent Cell Growth and Anoikis ResistanceAdvanced Science2024
      Zhang, Haokang et al.Helical vasculogenesis driven by cell chiralityScience Advances2024
      Grandy, Carolin et al.Remodeling of the focal adhesion complex by hydrogen-peroxide-induced senescenceScientific Reports2023
      González, Yasmilde Rodríguez et al.PFTK1 kinase regulates axogenesis during development via RhoA activationBMC Biology2023
      Ruffine, Valentin et al.Twofold Mechanosensitivity Ensures Actin Cortex Reinforcement upon Peaks in Mechanical TensionAdvanced Physics Research2023
      Wong, Darren Chen Pei et al.The scaffold RhoGAP protein ARHGAP8/BPGAP1 synchronizes Rac and Rho signaling to facilitate cell migrationMolecular Biology of the Cell2023
      Wong, Darren Chen Pei et al.Hiltonol, a dsRNA Mimic, Promotes NK Cell Anticancer Cytotoxicity Through TAZ Cytoplasmic SequestrationAdvanced Therapeutics2023
      Rübsam, Matthias et al.Polarity signaling balances epithelial contractility and mechanical resistanceScientific Reports 2023 13:12023
      Oh, Mijung et al.High extracellular glucose promotes cell motility by modulating cell deformability and contractility via the cAMP-RhoA-ROCK axis in human breast cancer cellsMolecular Biology of the Cell2023
      Aifuwa, Ivie et al.Senescent stroma induces nuclear deformations in cancer cells via the inhibition of RhoA/ROCK/myosin II-based cytoskeletal tensionPNAS Nexus2023
      Gutiérrez-Martínez, Enric et al.Actin-regulated Siglec-1 nanoclustering influences HIV-1 capture and virus-containing compartment formation in dendritic cellseLife2023
      Noviello, Chiara et al.RhoA within myofibers controls satellite cell microenvironment to allow hypertrophic growthiScience2022
      Wong, Darren Chen Pei et al.BNIP-2 Activation of Cellular Contractility Inactivates YAP for H9c2 Cardiomyoblast DifferentiationAdvanced Science2022
      Kim, Kyung Ah et al.Characterization of Integrin Molecular Tension of Human Breast Cancer Cells on Anisotropic NanopatternsFrontiers in Molecular Biosciences2022
      Leguay, Kévin et al.Interphase microtubule disassembly is a signaling cue that drives cell rounding at mitotic entryJournal of Cell Biology2022
      Hu, Xunwu et al.Control cell migration by engineering integrin ligand assemblyNature Communications 2022 13:12022
      Xu, Weiyi et al.Paxillin promotes breast tumor collective cell invasion through maintenance of adherens junction integrityhttps://doi.org/10.1091/mbc.E21-09-04322022
      Noviello, Chiara et al.RhoA within myofibers controls satellite cell microenvironment to allow hypertrophic growthiScience2022
      Hilfenhaus, Georg et al.A High-Content Screen Identifies Drugs That Restrict Tumor Cell Extravasation across the Endothelial BarrierCancer Research2021
      Laly, Ana C. et al.The keratin network of intermediate filaments regulates keratinocyte rigidity sensing and nuclear mechanotransductionScience Advances2021
      Saraswathibhatla, Aashrith et al.Coordinated tractions increase the size of a collectively moving pack in a cell monolayerExtreme Mechanics Letters2021
      Hoffmann, Lena et al.Cofilin1 oxidation links oxidative distress to mitochondrial demise and neuronal cell deathCell Death and Disease2021
      Li, Wenhong et al.Differential cellular responses to adhesive interactions with galectin-8- And fibronectin-coated substratesJournal of Cell Science2021
      Kim, Nayoung et al.Mitf promotes cell growth, migration and invasion in clear cell renal cell carcinoma by activating the rhoa/yap signal pathwayCancers2021
      Gaston, Cécile et al.EpCAM promotes endosomal modulation of the cortical RhoA zone for epithelial organizationNature Communications2021
      Wang, Yuan et al.LIMD1 phase separation contributes to cellular mechanics and durotaxis by regulating focal adhesion dynamics in response to forceDevelopmental Cell2021
      Eddy, Christopher Z. et al.Morphodynamics facilitate cancer cells to navigate 3D extracellular matrixScientific Reports2021
      Rong, Zhouyi et al.Activation of FAK/Rac1/Cdc42-GTPase signaling ameliorates impaired microglial migration response to Aβ42 in triggering receptor expressed on myeloid cells 2 loss-of-function murine modelsFASEB Journal2020
      Yu, Sun Min et al.Mechanical Adaptations of Epithelial Cells on Various Protruded Convex GeometriesCells2020
      Cheong, Sek Shir et al.The Planar Polarity Component VANGL2 Is a Key Regulator of MechanosignalingFrontiers in Cell and Developmental Biology2020
      Stankiewicz, Trisha R. et al.Corrigendum to “Dysregulation of Rac or Rho elicits death of motor neurons and activation of these GTPases is altered in the G93A mutant hSOD1 mouse model of amyotrophic lateral sclerosis” [Neurobiology of Disease 136 (2020) 104743] (Neurobiology of DiseaNeurobiology of Disease2020
      Adeniba, Olaoluwa O. et al.Simultaneous time-varying viscosity, elasticity, and mass measurements of single adherent cancer cells across cell cycleScientific Reports2020
      Flasse, Lydie et al.Apical Restriction of the Planar Cell Polarity Component VANGL in Pancreatic Ducts Is Required to Maintain Epithelial IntegrityCell Reports2020
      Xia, Mingyu et al.Activation of the RhoA-YAP-β-catenin signaling axis promotes the expansion of inner ear progenitor cells in 3D cultureStem Cells2020
      Bhosle, Vikrant K. et al.SLIT2/ROBO1-signaling inhibits macropinocytosis by opposing cortical cytoskeletal remodelingNature Communications2020
      Hernandez, Paula A. et al.Actomyosin contractility confers mechanoprotection against tnfα-induced disruption of the intervertebral discScience Advances2020
      Pan, Meng et al.BNIP-2 retards breast cancer cell migration by coupling microtubule-mediated GEF-H1 and RhoA activationScience Advances2020
      Thomas, Minnah et al.Desmosomal Junctions Govern Tissue Integrity and Actomyosin Contractility in Apoptotic Cell ExtrusionCurrent Biology2020
      Dias Gomes, Martim et al.Polarity signaling ensures epidermal homeostasis by coupling cellular mechanics and genomic integrityNature Communications2019
      Miao, Hui et al.Cell ratcheting through the Sbf RabGEF directs force balancing and stepped apical constrictionJournal of Cell Biology2019
      Huang, Yuxing et al.Arp2/3-branched actin maintains an active pool of GTP-RhoA and controls RhoA abundanceCells2019
      Rafiq, Nisha Bte Mohd et al.A mechano-signalling network linking microtubules, myosin IIA filaments and integrin-based adhesionsNature Materials2019
      Yong, Yu et al.p75NTR and DR6 regulate distinct phases of axon degeneration demarcated by spheroid ruptureJournal of Neuroscience2019
      Mistriotis, Panagiotis et al.Confinement hinders motility by inducing RhoA-mediated nuclear influx, volume expansion, and blebbingJournal of Cell Biology2019
      Shu, Liang et al.Brain ischemic insult induces cofilin rod formation leading to synaptic dysfunction in neuronsJournal of Cerebral Blood Flow and Metabolism2019
      Kalinski, Ashley L. et al.Deacetylation of Miro1 by HDAC6 blocks mitochondrial transport and mediates axon growth inhibitionJournal of Cell Biology2019
      Zhao, Meng et al.Enhancing the engraftment of human induced pluripotent stem cell-derived cardiomyocytes via a transient inhibition of rho kinase activityJournal of Visualized Experiments2019
      Mosier, Jenna A. et al.Extent of Cell Confinement in Microtracks Affects Speed and Results in Differential Matrix StrainsBiophysical Journal2019
      Eliazer, Susan et al.Wnt4 from the Niche Controls the Mechano-Properties and Quiescent State of Muscle Stem CellsCell Stem Cell2019
      Zanotelli, Matthew R. et al.Energetic costs regulated by cell mechanics and confinement are predictive of migration path during decision-makingNature Communications2019
      Rangel, Laura et al.Caveolin-1α regulates primary cilium length by controlling RhoA GTPase activityScientific Reports2019
      Zhang, Qiao et al.Mechanical Stabilization of the Glandular Acinus by Linker of Nucleoskeleton and Cytoskeleton ComplexCurrent Biology2019
      Roxas, Jennifer Lising et al.Enteropathogenic Escherichia coli EspH-Mediated Rho GTPase Inhibition Results in Desmosomal PerturbationsCellular and Molecular Gastroenterology and Hepatology2018
      Shiu, Jau Ye et al.Nanopillar force measurements reveal actin-cap-mediated YAP mechanotransductionNature Cell Biology2018
      Rahman-Zaman, Aniqua et al.Cell Migration in Microfabricated 3D Collagen Microtracks is Mediated Through the Prometastatic Protein GirdinCellular and Molecular Bioengineering2018
      Jones, Matthew C. et al.Cell adhesion is regulated by CDK1 during the cell cycleJournal of Cell Biology2018
      Freeman, Spencer A. et al.Transmembrane Pickets Connect Cyto- and Pericellular Skeletons Forming Barriers to Receptor EngagementCell2018
      Huang, Chao et al.Tetraspanin-enriched microdomains regulate digitation junctionsCellular and Molecular Life Sciences2018
      Herbert, Lindsay M. et al.RhoA increases ASIC1a plasma membrane localization and calcium influx in pulmonary arterial smooth muscle cells following chronic hypoxiaAmerican Journal of Physiology - Cell Physiology2018
      Werner, Craig T. et al.E3 Ubiquitin-Protein Ligase SMURF1 in the Nucleus Accumbens Mediates Cocaine SeekingBiological Psychiatry2018
      Han, Han et al.Regulation of the Hippo Pathway by Phosphatidic Acid-Mediated Lipid-Protein InteractionMolecular Cell2018
      Benedicto, Ignacio et al.Concerted regulation of retinal pigment epithelium basement membrane and barrier function by angiocrine factorsNature Communications2017
      Widmeier, Eugen et al.A small molecule screening to detect potential therapeutic targets in human podocytesAmerican Journal of Physiology - Renal Physiology2017
      Bade, Nathan D. et al.Curvature and Rho activation differentially control the alignment of cells and stress fibersScience Advances2017
      Lázaro-Diéguez, Francisco et al.Cell-cell adhesion accounts for the different orientation of columnar and hepatocytic cell divisionsJournal of Cell Biology2017
      Hirata, Hiroaki et al.Actomyosin contractility provokes contact inhibition in E-cadherin-ligated keratinocytesScientific Reports2017
      Li, Yao et al.Rho kinase activity governs arteriolar myogenic depolarizationJournal of Cerebral Blood Flow and Metabolism2017
      Wu, Mengrui et al.Gα13 negatively controls osteoclastogenesis through inhibition of the Akt-GSK3β-NFATc1 signalling pathwayNature Communications2017
      Daoud, Abdelkader et al.Molecular and functional crosstalk between extracellular Hsp90 and ephrin A1 signalingOncotarget2017
      Hamze-Komaiha, Ola et al.SHIP2 Regulates Lumen Generation, Cell Division, and Ciliogenesis through the Control of Basolateral to Apical Lumen Localization of Aurora A and HEF 1Cell Reports2016
      Yu, Yonghao et al.Hydrogen-rich medium ameliorates lipopolysaccharide-induced barrier dysfunction via rhoa-mdia1 signaling in caco-2 cellsShock2016
      López-Posadas, Rocío et al.Rho-A prenylation and signaling link epithelial homeostasis to intestinal inflammationJournal of Clinical Investigation2016
      Agbor, Larry N. et al.Cullin-3 mutation causes arterial stiffness and hypertension through a vascular smooth muscle mechanismJCI Insight2016
      Jackson, William D. et al.Very-low and low-density lipoproteins induce neutral lipid accumulation and impair migration in monocyte subsetsScientific Reports2016
      Sayedyahossein, Samar et al.Integrin-Linked Kinase Is Indispensable for Keratinocyte Differentiation and Epidermal Barrier FunctionJournal of Investigative Dermatology2016
      Takito, Jiro et al.Regulation of Osteoclast Multinucleation by the Actin Cytoskeleton Signaling NetworkJournal of cellular physiology2015
      Bhandary, Lekhana et al.ROCK inhibition promotes microtentacles that enhance reattachment of breast cancer cellsOncotarget2015
      Lahne, Manuela et al.Actin-cytoskeleton-and rock-mediated inm are required for photoreceptor regeneration in the adult zebrafish retinaJournal of Neuroscience2015
      Freeman, Spencer A. et al.Toll-like receptor ligands sensitize B-cell receptor signalling by reducing actin-dependent spatial confinement of the receptorNature Communications2015
      Lee, Meng Horng et al.Normal mammary epithelial cells promote carcinoma basement membrane invasion by inducing microtubule-rich protrusionsOncotarget2015
      Aifuwa, Ivie et al.Senescent stromal cells induce cancer cell migration via inhibition of RhoA/ROCK/myosin-based cell contractilityOncotarget2015
      Herr, Michael J. et al.Tetraspanin CD9 regulates cell contraction and actin arrangement via RhoA in human vascular smooth muscle cellsPLoS ONE2014
      Sun, Shan et al.Impact of oxidative stress on cellular biomechanics and rho signaling in C2C12 myoblastsJournal of biomechanics2014
      Lavall, Daniel et al.The mineralocorticoid receptor promotes fibrotic remodeling in atrial fibrillationJournal of Biological Chemistry2014
      De Vega, Susana et al.A C-terminal fragment of fibulin-7 interacts with endothelial cells and inhibits their tube formation in cultureArchives of Biochemistry and Biophysics2014
      Iyer, Padma et al.Connective tissue growth factor-mediated upregulation of neuromedin U expression in trabecular meshwork cells and its role in homeostasis of aqueous humor outflowInvestigative Ophthalmology and Visual Science2012
      Kuang, Shao Qing et al.Rare, nonsynonymous variant in the smooth muscle-specific isoform of myosin heavy chain, MYH11, R247C, alters force generation in the aorta and phenotype of smooth muscle cellsCirculation Research2012
      Pignatelli, Jeanine et al.Actopaxin (α-parvin) phosphorylation is required for matrix degradation and cancer cell invasionJournal of Biological Chemistry2012

      Question 1:  Can the direct Rho activator CN03 be used with cells growing in culture?

      Answer 1:  Yes, CN03 is specifically designed to be used as a Rho activator with cultured cells.  The active site of CN03 is based on the catalytic domain of the bacterial cytotoxic necrotizing factor (CNF) toxins.  The catalytic domain of CN03 is covalently attached to a proprietary cell penetrating moiety.  Upon entry into the cell, CN03 activates Rho GTPase isoforms by deamidating glutamine-63, which is located in the Switch II region of these GTPases.  This modification converts glutamine-63 to glutamate, which blocks intrinsic and GAP-stimulated GTPase activity, resulting in constitutively active Rho.  CN03 robustly increases the level of GTP-bound RhoA within 2-4 h after addition to the culture medium.  

       

      Question 2:  How can I assess whether Rho activity is changing in my cells following CN03 treatment? 

      Answer 2:  There are multiple ways to measure changes in Rho activity.  To visualize a change in Rho activity, we recommend examining Rho-mediated stress fiber formation with fluorescently-labeled phalloidin (Cat. # PHDG1, PHDH1, PHDN1, PHDR1).  These Acti-stain phalloidins label F-actin stress fibers.  Activation of Rho can be directly quantified with one of our activation assays, either the traditional pull-down (Cat. # BK036) or the RhoA G-LISA activation assay (Cat. # BK124). 

       

       If you have any questions concerning this product, please contact our Technical Service department at tservice@cytoskeleton.com.

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