Home / Rho GTPase Inhibitors / NSC 23766

NSC 23766

Catalog #: 2161
56 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
2161/10
2161/50
NSC 23766 | CAS No. 1177865-17-6 | Rho GTPase Inhibitors
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Description: Selective inhibitor of Rac1-GEF interaction; antioncogenic

Chemical Name: N6-[2-[[4-(Diethylamino)-1-methylbutyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-quinolinediamine trihydrochloride

Purity: ≥99%

Product Details
Citations (56)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

NSC 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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. LPA, HGF, and EGF utilize distinct combinations of signaling pathways to promote migration and invasion of MDA-MB-231 breast carcinoma cells.
    Harrison, Susan M, Knifley, Teresa, Chen, Min, O'Connor, Kathleen
    BMC Cancer, 2013;13(0):501.
  2. The P2X7 receptor is an upstream regulator of dynamic blebbing and a pluripotency marker in human embryonic stem cells
    NJ Weng, P Talbot
    Stem Cell Res, 2017;23(0):39-49.
  3. VE-Cadherin Disassembly and Cell Contractility in the Endothelium are Necessary for Barrier Disruption Induced by Tumor Cells
    V Aragon-San, SE Pohler, VJ Eswar, M Bierowski, EW Gomez, C Dong
    Sci Rep, 2017;7(0):45835.
  4. Mesothelial cells promote early ovarian cancer metastasis through fibronectin secretion.
    Kenny H, Chiang C, White E, Schryver E, Habis M, Romero I, Ladanyi A, Penicka C, George J, Matlin K, Montag A, Wroblewski K, Yamada S, Mazar A, Bowtell D, Lengyel E
    J Clin Invest, 2014;124(10):4614-28.
  5. TIPE2 controls innate immunity to RNA by targeting the phosphatidylinositol 3-kinase-rac pathway.
    Sun H, Zhuang G, Chai L, Wang Z, Johnson D, Ma Y, Chen Y
    J Immunol, 2012;189(6):2768-73.
  6. Myeloid-derived tissue-type plasminogen activator promotes macrophage motility through FAK, Rac1, and NF-kappaB pathways.
    Lin L, Jin Y, Mars W, Reeves W, Hu K
    Am J Pathol, 2014;184(10):2757-67.
  7. Bladder cancer extracellular vesicles drive tumorigenesis by�inducing the unfolded protein response in endoplasmic reticulum of non-malignant cells
    CH Wu, CR Silvers, EM Messing, YF Lee
    J. Biol. Chem., 2018;0(0):.
  8. Involvement of Rac in thromboxane A2induced human platelet activation: regulation of sCD40 ligand release and PDGFAB secretion.
    Kageyama Y, Doi T, Matsushima-Nishiwaki R, Iida Y, Akamatsu S, Kondo A, Kuroyanagi G, Yamamoto N, Mizutani J, Otsuka T, Tokuda H, Iida H, Kozawa O, Ogura S
    Mol Med Rep, 2014;10(1):107-12.
  9. Overexpression of developmentally regulated GTP-binding protein-2 increases bone loss.
    Ke K, Sul O, Kim W, Lee M, Ko M, Suh J, Kim H, Kim S, Park J, Choi H
    Am J Physiol Endocrinol Metab, 2013;304(7):E703-10.
  10. Inter-cellular exchange of cellular components via VE-cadherin-dependent trans-endocytosis.
    Sakurai T, Woolls M, Jin S, Murakami M, Simons M
    PLoS ONE, 2014;9(6):e90736.
  11. Protein tyrosine phosphatase-PEST and beta8 integrin regulate spatiotemporal patterns of RhoGDI1 activation in migrating cells.
    Lee H, Cheerathodi M, Chaki S, Reyes S, Zheng Y, Lu Z, Paidassi H, DerMardirossian C, Lacy-Hulbert A, Rivera G, McCarty J
    Mol Cell Biol, 2015;35(8):1401-13.

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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

  1. Non-canonical Wnt signaling regulates junctional mechanocoupling during angiogenic collective cell migration.
    Authors: Carvalho Et al.
    Elife  2019;8
  2. 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
  3. Matrix mechanical plasticity regulates cancer cell migration through confining microenvironments.
    Authors: Wisdom Et al.
    Nat Commun  2018;9:4144
  4. Chlamydia exploits filopodial capture and a macropinocytosis-like pathway for host cell entry.
    Authors: Ford Et al.
    PLoS Pathog  2018;14:e1007051
  5. In vivo imaging of emerging endocrine cells reveals a requirement for PI3K-regulated motility in pancreatic islet morphogenesis.
    Authors: Freudenblum Et al.
    Development  2018;145
  6. 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;
  7. Concerted regulation of retinal pigment epithelium basement membrane and barrier function by angiocrine factors.
    Authors: Benedicto
    Nat Commun  2017;8:15374
  8. Paxillin facilitates timely neurite initiation on soft-substrate environments by interacting with the endocytic machinery.
    Authors: Chang Et al.
    Elife  2017;6
  9. 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
  10. 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.
    Virulence  2016;7:806
  11. 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
  12. N-cadherin adhesive interactions modulate matrix mechanosensing and fate commitment of mesenchymal stem cells.
    Authors: Cosgrove
    Nature Materials  2016;15:1297
  13. 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
  14. 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
  15. 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
  16. Endothelial Rac1 is essential for hematogenous metastasis to the lung.
    Authors: Yao Et al.
    Sci Rep  2015;6:17501
  17. 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
  18. proBDNF and p75NTR Control Excitability and Persistent Firing of Cortical Pyramidal Neurons.
    Authors: Gibon Et al.
    J Neurosci  2015;35:9741
  19. EP2 Induces p38 Phosphorylation via the Activation of Src in HEK 293 Cells.
    Authors: Chun and Shim
    Oncotarget  2015;23:539
  20. 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
  21. 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
  22. 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
  23. Architecture and migration of an epithelium on a cylindrical wire.
    Authors: Yevick Et al.
    Nat Commun  2015;112:5944
  24. 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
  25. 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
  26. Gasdermin-B promotes invasion and metastasis in breast cancer cells.
    Authors: Hergueta-Redondo Et al.
    PLoS One  2014;9:e90099
  27. Coxsackievirus A9 infects cells via nonacidic multivesicular bodies.
    Authors: Huttunen Et al.
    J Virol  2014;88:5138
  28. 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
  29. The Rac1 inhibitor NSC23766 suppresses CREB signaling by targeting NMDA receptor function.
    Authors: Hou Et al.
    J Neurosci  2014;34:14006
  30. Specific phosphorylations transmit signals from leukocyte β2 to β1 integrins and regulate adhesion.
    Authors: Uotila Et al.
    J Cell Biol  2014;289:32230
  31. 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
  32. CDC-42 and RAC-1 regulate opposite chemotropisms in Neurospora crassa.
    Authors: Lichius Et al.
    J Cell Sci  2014;127:1953
  33. Mesothelial cells promote early ovarian cancer metastasis through fibronectin secretion.
    Authors: Kenny Et al.
    J Clin Invest  2014;124:4614
  34. Inhibition of Rac and ROCK signalling influence osteoblast adhesion, differentiation and mineralization on titanium topographies.
    Authors: Prowse Et al.
    PLoS One  2013;8:e58898
  35. Rac1 and Cdc42 GTPases regulate shear stress-driven β-catenin signaling in osteoblasts.
    Authors: Wan Et al.
    Biochem Biophys Res Commun  2013;433:502
  36. PI3K regulates branch initiation and extension of cultured mammary epithelia via Akt and Rac1 respectively.
    Authors: Zhu and Nelson
    Cancer Res  2013;379:235
  37. Par3 controls neural crest migration by promoting microtubule catastrophe during contact inhibition of locomotion.
    Authors: Moore Et al.
    Development  2013;140:4763
  38. 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
  39. 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
  40. Pak and Rac GTPases promote oncogenic KIT-induced neoplasms.
    Authors: Martin Et al.
    J Clin Invest  2013;123:4449
  41. 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
  42. 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;
  43. Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior.
    Authors: Tseng Et al.
    Oncotarget  2012;9:1113
  44. Inhibition of hepcidin transcription by growth factors.
    Authors: Goodnough Et al.
    Hepatology  2012;56:291
  45. Activation of canonical Wnt signalling is required for TGF-β-mediated fibrosis.
    Authors: Akhmetshina Et al.
    Biomol Ther (Seoul)  2012;3:735
  46. ROCK1 feedback regulation of the upstream small GTPase RhoA.
    Authors: Tang Et al.
    Cell Signal  2012;24:1375
  47. Cadherin point mutations alter cell sorting and modulate GTPase signaling.
    Authors: Tabdili Et al.
    J Cell Sci  2012;125:3299
  48. 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
  49. Activity of the RhoU/Wrch1 GTPase is critical for cranial neural crest cell migration.
    Authors: Fort Et al.
    Dev Biol  2011;350:451
  50. TCR-induced activation of LFA-1 involves signaling through Tiam1.
    Authors: Grönholm Et al.
    J Immunol  2011;187:3613
  51. 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
  52. P190B RhoGAP has pro-tumorigenic functions during MMTV-Neu mammary tumorigenesis and metastasis.
    Authors: McHenry Et al.
    Breast Cancer Res  2010;12:R73
  53. Tissue geometry patterns epithelial-mesenchymal transition via intercellular mechanotransduction.
    Authors: Gomez Et al.
    Nat Methods  2010;110:44
  54. 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
  55. 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
  56. 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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