Chemical Name: N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride
Biological ActivitySelective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) TrioN and Tiam1 (IC50 ~ 50 μM) without affecting Cdc42 or RhoA activation. Inhibits Rac1-mediated cell functions and is reported to reverse tumor cell phenotypes in prostate cancer cells.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Rational design and characterization of a Rac GTPase-specific small molecule inhibitor.
Gao et al.
Citations for NSC 23766
The citations listed below are publications that use Tocris products. Selected citations for NSC 23766 include:
56 Citations: Showing 1 - 10
Non-canonical Wnt signaling regulates junctional mechanocoupling during angiogenic collective cell migration.
Authors: Carvalho Et al.
RAC1P29S Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance.
Authors: Lionarons Et al.
Cancer Cell 2019;36:68
Matrix mechanical plasticity regulates cancer cell migration through confining microenvironments.
Authors: Wisdom Et al.
Nat Commun 2018;9:4144
Chlamydia exploits filopodial capture and a macropinocytosis-like pathway for host cell entry.
Authors: Ford Et al.
PLoS Pathog 2018;14:e1007051
In vivo imaging of emerging endocrine cells reveals a requirement for PI3K-regulated motility in pancreatic islet morphogenesis.
Authors: Freudenblum Et al.
Bladder cancer extracellular vesicles drive tumorigenesis by inducing the unfolded protein response in endoplasmic reticulum of non-malignant cells.
Authors: Wu Et al.
J Biol Chem 2018;
Concerted regulation of retinal pigment epithelium basement membrane and barrier function by angiocrine factors.
Nat Commun 2017;8:15374
Paxillin facilitates timely neurite initiation on soft-substrate environments by interacting with the endocytic machinery.
Authors: Chang Et al.
The Small GTPase Rac1 Contributes to Extinction of Aversive Memories of Drug Withdrawal by Facilitating GABAA Receptor Endocytosis in the vmPFC.
Authors: Wang Et al.
J Neurosci 2017;37:7096
The effects of cytotoxic necrotizing factor 1 expression in the uptake of Escherichia coli K1 by macrophages and the onset of meningitis in newborn mice.
Authors: Chang Et al.
WNT5a is required for normal ovarian follicle development and antagonizes g.tropin responsiveness in granulosa cells by suppressing canonical WNT signaling.
Authors: Abedini Et al.
FASEB J 2016;30:1534
N-cadherin adhesive interactions modulate matrix mechanosensing and fate commitment of mesenchymal stem cells.
Nature Materials 2016;15:1297
Post-training activation of Rac1 in the basolateral amygdala is required for the formation of both short-term and long-term auditory fear memory.
Authors: Gao Et al.
Stem Cell Res Ther 2015;8:65
Migration of germline progenitor cells is directed by sphingosine-1-phosphate signalling in a basal chordate.
Authors: Kassmer Et al.
Nat Commun 2015;6:8565
Synergism of MSC-secreted HGF and VEGF in stabilising endothelial barrier function upon lipopolysaccharide stimulation via the Rac1 pathway.
Authors: Yang Et al.
Proc Natl Acad Sci U S A 2015;6:250
Endothelial Rac1 is essential for hematogenous metastasis to the lung.
Authors: Yao Et al.
Sci Rep 2015;6:17501
PAK2 is an effector of TSC1/2 signaling independent of mTOR and a potential therapeutic target for Tuberous Sclerosis Complex.
Authors: Alves Et al.
Front Mol Neurosci 2015;5:14534
proBDNF and p75NTR Control Excitability and Persistent Firing of Cortical Pyramidal Neurons.
Authors: Gibon Et al.
J Neurosci 2015;35:9741
EP2 Induces p38 Phosphorylation via the Activation of Src in HEK 293 Cells.
Authors: Chun and Shim
Competition for actin between two distinct F-actin networks defines a bistable switch for cell polarization.
Authors: Lomakin Et al.
Nat Cell Biol 2015;17:1435
Inhibition of prostate smooth muscle contraction and prostate stromal cell growth by the inhibitors of Rac, NSC23766 and EHT1864.
Authors: Wang Et al.
Br J Pharmacol 2015;172:2905
Rac1 and ROCK are implicated in the cell surface delivery of GLUT4 under the control of the Ins signal mimetic diDCP-LA-PE.
Authors: Tsuchiya Et al.
J Pharmacol Sci 2015;128:179
Architecture and migration of an epithelium on a cylindrical wire.
Authors: Yevick Et al.
Nat Commun 2015;112:5944
Antioxidant Treatment and Induction of Autophagy Cooperate to Reduce Desmin Aggregation in a Cellular Model of Desminopathy.
Authors: Cabet Et al.
PLoS One 2015;10:e0137009
SimV. Increases Fibulin-2 Expression in Human Coronary Artery Smooth Muscle Cells via RhoA/Rho-Kinase Signaling Pathway Inhibition.
Authors: Serra Et al.
PLoS One 2015;10:e0133875
Gasdermin-B promotes invasion and metastasis in breast cancer cells.
Authors: Hergueta-Redondo Et al.
PLoS One 2014;9:e90099
Coxsackievirus A9 infects cells via nonacidic multivesicular bodies.
Authors: Huttunen Et al.
J Virol 2014;88:5138
Rac1 regulates skin tumors by regulation of keratin 17 through recruitment and interaction with CD11b+Gr1+ cells.
Authors: Chen Et al.
J Biol Chem 2014;5:4406
The Rac1 inhibitor NSC23766 suppresses CREB signaling by targeting NMDA receptor function.
Authors: Hou Et al.
J Neurosci 2014;34:14006
Specific phosphorylations transmit signals from leukocyte β2 to β1 integrins and regulate adhesion.
Authors: Uotila Et al.
J Cell Biol 2014;289:32230
Transforming growth factor β-induced superficial zone protein accumulation in the surface zone of articular cartilage is dependent on the cytoskeleton.
Authors: McNary Et al.
Tissue Eng Part A 2014;20:921
CDC-42 and RAC-1 regulate opposite chemotropisms in Neurospora crassa.
Authors: Lichius Et al.
J Cell Sci 2014;127:1953
Mesothelial cells promote early ovarian cancer metastasis through fibronectin secretion.
Authors: Kenny Et al.
J Clin Invest 2014;124:4614
Inhibition of Rac and ROCK signalling influence osteoblast adhesion, differentiation and mineralization on titanium topographies.
Authors: Prowse Et al.
PLoS One 2013;8:e58898
Rac1 and Cdc42 GTPases regulate shear stress-driven β-catenin signaling in osteoblasts.
Authors: Wan Et al.
Biochem Biophys Res Commun 2013;433:502
PI3K regulates branch initiation and extension of cultured mammary epithelia via Akt and Rac1 respectively.
Authors: Zhu and Nelson
Cancer Res 2013;379:235
Par3 controls neural crest migration by promoting microtubule catastrophe during contact inhibition of locomotion.
Authors: Moore Et al.
LPA, HGF, and EGF utilize distinct combinations of signaling pathways to promote migration and invasion of MDA-MB-231 breast carcinoma cells.
Authors: Harrison Et al.
BMC Cancer 2013;13:501
Involvement of Botrytis cinerea small GTPases BcRAS1 and BcRAC in differentiation, virulence, and the cell cycle.
Authors: Dub Et al.
Eukaryot Cell 2013;12:1609
Pak and Rac GTPases promote oncogenic KIT-induced neoplasms.
Authors: Martin Et al.
J Clin Invest 2013;123:4449
Clostridium difficile toxin B-induced necrosis is mediated by the host epithelial cell NADPH oxidase complex.
Authors: Farrow Et al.
Proc Natl Acad Sci U S A 2013;110:18674
Inhibition of Rac1 activity by controlled release of NSC23766 from chitosan microspheres effectively ameliorates osteoarthritis development in vivo.
Authors: Zhu Et al.
Ann Rheum Dis 2013;
Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior.
Authors: Tseng Et al.
Inhibition of hepcidin transcription by growth factors.
Authors: Goodnough Et al.
Activation of canonical Wnt signalling is required for TGF-β-mediated fibrosis.
Authors: Akhmetshina Et al.
Biomol Ther (Seoul) 2012;3:735
ROCK1 feedback regulation of the upstream small GTPase RhoA.
Authors: Tang Et al.
Cell Signal 2012;24:1375
Cadherin point mutations alter cell sorting and modulate GTPase signaling.
Authors: Tabdili Et al.
J Cell Sci 2012;125:3299
mTORC1 and mTORC2 regulate EMT, motility, and metastasis of colorectal cancer via RhoA and Rac1 signaling pathways.
Authors: Gulhati Et al.
J Transl Med 2011;71:3246
Activity of the RhoU/Wrch1 GTPase is critical for cranial neural crest cell migration.
Authors: Fort Et al.
Dev Biol 2011;350:451
TCR-induced activation of LFA-1 involves signaling through Tiam1.
Authors: Grönholm Et al.
J Immunol 2011;187:3613
Rac1-mediated signaling plays a central role in secretion-dependent platelet aggregation in human blood stimulated by atherosclerotic plaque.
Authors: Dwivedi Et al.
Sci Rep 2010;8:128
P190B RhoGAP has pro-tumorigenic functions during MMTV-Neu mammary tumorigenesis and metastasis.
Authors: McHenry Et al.
Breast Cancer Res 2010;12:R73
Tissue geometry patterns epithelial-mesenchymal transition via intercellular mechanotransduction.
Authors: Gomez Et al.
Nat Methods 2010;110:44
NADPH oxidase and lipid raft-associated redox signaling are required for PCB153-induced upregulation of cell adhesion molecules in human brain endothelial cells.
Authors: Eum Et al.
Toxicol Appl Pharmacol 2009;240:299
Different Rho GTPase-dependent signaling pathways initiate sequential steps in the consolidation of long-term potentiation.
Authors: Rex Et al.
Dev Biol 2009;186:85
Characterization of Salmonella enterica serovar Typhimurium DT104 invasion in an epithelial cell line (IPEC J2) from porcine small intestine.
Authors: Brown and Price
Vet Microbiol 2007;120:328
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Rac specific inhibitor