Catalog Number: 2161
Chemical Name: N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride
Biological Activity
Selective 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 phenotyes in prostate cancer cells.
Technical Data
  • M.Wt:
    530.97
  • Formula:
    C24H35N7.3HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Desiccate at RT
  • CAS No:
    1177865-17-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Rational design and characterization of a Rac GTPase-specific small molecule inhibitor.
    Gao et al.
    Proc.Natl.Acad.Sci.USA, 2004;101:7618
Citations:

The citations listed below are publications that use Tocris products. Selected citations for NSC 23766 include:

35 Citations: Showing 1 - 10
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  1. Concerted regulation of retinal pigment epithelium basement membrane and barrier function by angiocrine factors.
    Authors: Benedicto
    Nat Commun 2017;8:15374
  2. N-cadherin adhesive interactions modulate matrix mechanosensing and fate commitment of mesenchymal stem cells.
    Authors: Cosgrove
    Nature Materials 2016;15:1297
  3. 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
  4. 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
  5. Endothelial Rac1 is essential for hematogenous metastasis to the lung.
    Authors: Yao Et al.
    Sci Rep 2015;6:17501
  6. 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
  7. EP2 Induces p38 Phosphorylation via the Activation of Src in HEK 293 Cells.
    Authors: Chun and Shim
    Oncotarget 2015;23:539
  8. Architecture and migration of an epithelium on a cylindrical wire.
    Authors: Yevick Et al.
    Nat Commun 2015;112:5944
  9. Simvastatin 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
  10. Gasdermin-B promotes invasion and metastasis in breast cancer cells.
    Authors: Hergueta-Redondo Et al.
    PLoS One 2014;9:e90099
  11. Coxsackievirus A9 infects cells via nonacidic multivesicular bodies.
    Authors: Huttunen Et al.
    J Virol 2014;88:5138
  12. 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
  13. The Rac1 inhibitor NSC23766 suppresses CREB signaling by targeting NMDA receptor function.
    Authors: Hou Et al.
    J Neurosci 2014;34:14006
  14. Specific phosphorylations transmit signals from leukocyte β2 to β1 integrins and regulate adhesion.
    Authors: Uotila Et al.
    J Cell Biol 2014;289:32230
  15. 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
  16. Mesothelial cells promote early ovarian cancer metastasis through fibronectin secretion.
    Authors: Kenny Et al.
    J Clin Invest 2014;124:4614
  17. Rac1 and Cdc42 GTPases regulate shear stress-driven β-catenin signaling in osteoblasts.
    Authors: Wan Et al.
    Biochem Biophys Res Commun 2013;433:502
  18. PI3K regulates branch initiation and extension of cultured mammary epithelia via Akt and Rac1 respectively.
    Authors: Zhu and Nelson
    Cancer Res 2013;379:235
  19. Par3 controls neural crest migration by promoting microtubule catastrophe during contact inhibition of locomotion.
    Authors: Moore Et al.
    Development 2013;140:4763
  20. 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
  21. 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
  22. Pak and Rac GTPases promote oncogenic KIT-induced neoplasms.
    Authors: Martin Et al.
    J Clin Invest 2013;123:4449
  23. 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
  24. 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;
  25. Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior.
    Authors: Tseng Et al.
    Oncotarget 2012;9:1113
  26. Inhibition of hepcidin transcription by growth factors.
    Authors: Goodnough Et al.
    Hepatology 2012;56:291
  27. Activation of canonical Wnt signalling is required for TGF-β-mediated fibrosis.
    Authors: Akhmetshina Et al.
    Biomol Ther (Seoul) 2012;3:735
  28. ROCK1 feedback regulation of the upstream small GTPase RhoA.
    Authors: Tang Et al.
    Cell Signal 2012;24:1375
  29. Cadherin point mutations alter cell sorting and modulate GTPase signaling.
    Authors: Tabdili Et al.
    J Cell Sci 2012;125:3299
  30. 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
  31. TCR-induced activation of LFA-1 involves signaling through Tiam1.
    Authors: Grönholm Et al.
    J Immunol 2011;187:3613
  32. 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
  33. Tissue geometry patterns epithelial-mesenchymal transition via intercellular mechanotransduction.
    Authors: Gomez Et al.
    Nat Methods 2010;110:44
  34. 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
  35. 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
Expand to show all 35 Citations

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