Chemical Name: N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride
Biological ActivityNSC 23766 is a selective inhibitor of Rac1-GEF interaction. NSC 23766 prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) TrioN and Tiam1 (IC50 ~ 50 μM) without affecting Cdc42 or RhoA activation. The compound inhibits Rac1-mediated cell functions and is reported to reverse tumor cell phenotypes in prostate cancer cells. NSC 23766 also inhibits mammary carcinoma cell invasion in vitro and inhibits mammary tumor progression and metastasis in a mouse model.
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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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