NSC 23766

Cat. No. 2161

NSC 23766 C24H35N7.3HCl [1177865-17-6]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Gao et al (2004) Rational design and characterization of a Rac GTPase-specific small molecule inhibitor. Proc.Natl.Acad.Sci.USA 101 7618.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for NSC 23766 include:

Alves et al (2015) PAK2 is an effector of TSC1/2 signaling independent of mTOR and a potential therapeutic target for Tuberous Sclerosis Complex. Front Mol Neurosci 5 14534. PMID: 26412398.

Chun and Shim (2015) EP2 Induces p38 Phosphorylation via the Activation of Src in HEK 293 Cells. Oncotarget 23 539. PMID: 26535079.

Gao et al (2015) Post-training activation of Rac1 in the basolateral amygdala is required for the formation of both short-term and long-term auditory fear memory. Stem Cell Res Ther 8 65. PMID: 26582975.

Serra et al (2015) Simvastatin Increases Fibulin-2 Expression in Human Coronary Artery Smooth Muscle Cells via RhoA/Rho-Kinase Signaling Pathway Inhibition. PLoS One 10 e0133875. PMID: 26207907.

Yang et al (2015) Synergism of MSC-secreted HGF and VEGF in stabilising endothelial barrier function upon lipopolysaccharide stimulation via the Rac1 pathway. Proc Natl Acad Sci U S A 6 250. PMID: 26674641.

Yao et al (2015) Endothelial Rac1 is essential for hematogenous metastasis to the lung. Sci Rep 6 17501. PMID: 25991673.

Yevick et al (2015) Architecture and migration of an epithelium on a cylindrical wire. Nat Commun 112 5944. PMID: 25922533.

Chen et al (2014) Rac1 regulates skin tumors by regulation of keratin 17 through recruitment and interaction with CD11b+Gr1+ cells. J Biol Chem 5 4406. PMID: 24962779.

Hergueta-Redondo et al (2014) Gasdermin-B promotes invasion and metastasis in breast cancer cells. PLoS One 9 e90099. PMID: 24675552.

Hou et al (2014) The Rac1 inhibitor NSC23766 suppresses CREB signaling by targeting NMDA receptor function. J Neurosci 34 14006. PMID: 25319697.

Huttunen et al (2014) Coxsackievirus A9 infects cells via nonacidic multivesicular bodies. J Virol 88 5138. PMID: 24574401.

Kenny et al (2014) Mesothelial cells promote early ovarian cancer metastasis through fibronectin secretion. J Clin Invest 124 4614. PMID: 25202979.

McNary et al (2014) Transforming growth factor β-induced superficial zone protein accumulation in the surface zone of articular cartilage is dependent on the cytoskeleton. Tissue Eng Part A 20 921. PMID: 24116978.

Uotila et al (2014) Specific phosphorylations transmit signals from leukocyte β2 to β1 integrins and regulate adhesion. J Cell Biol 289 32230. PMID: 25278023.

Dub et al (2013) Involvement of Botrytis cinerea small GTPases BcRAS1 and BcRAC in differentiation, virulence, and the cell cycle. Eukaryot Cell 12 1609. PMID: 24096906.

Farrow et al (2013) Clostridium difficile toxin B-induced necrosis is mediated by the host epithelial cell NADPH oxidase complex. Proc Natl Acad Sci U S A 110 18674. PMID: 24167244.

Harrison et al (2013) LPA, HGF, and EGF utilize distinct combinations of signaling pathways to promote migration and invasion of MDA-MB-231 breast carcinoma cells. BMC Cancer 13 501. PMID: 24160245.

Martin et al (2013) Pak and Rac GTPases promote oncogenic KIT-induced neoplasms. J Clin Invest 123 4449. PMID: 24091327.

Moore et al (2013) Par3 controls neural crest migration by promoting microtubule catastrophe during contact inhibition of locomotion. Development 140 4763. PMID: 24173803.

Wan et al (2013) Rac1 and Cdc42 GTPases regulate shear stress-driven β-catenin signaling in osteoblasts. Biochem Biophys Res Commun 433 502. PMID: 23524265.

Zhu et al (2013) Inhibition of Rac1 activity by controlled release of NSC23766 from chitosan microspheres effectively ameliorates osteoarthritis development in vivo. Ann Rheum Dis. PMID: 24257023.

Zhu and Nelson (2013) PI3K regulates branch initiation and extension of cultured mammary epithelia via Akt and Rac1 respectively. Cancer Res 379 235. PMID: 23665174.

Akhmetshina et al (2012) Activation of canonical Wnt signalling is required for TGF-β-mediated fibrosis. Biomol Ther (Seoul) 3 735. PMID: 22415826.

Goodnough et al (2012) Inhibition of hepcidin transcription by growth factors. Hepatology 56 291. PMID: 22278715.

Tabdili et al (2012) Cadherin point mutations alter cell sorting and modulate GTPase signaling. J Cell Sci 125 3299. PMID: 22505612.

Tang et al (2012) ROCK1 feedback regulation of the upstream small GTPase RhoA. Cell Signal 24 1375. PMID: 22430126.

Tseng et al (2012) Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior. Oncotarget 9 1113. PMID: 23064517.

Grönholm et al (2011) TCR-induced activation of LFA-1 involves signaling through Tiam1. J Immunol 187 3613. PMID: 21876037.

Gulhati et al (2011) mTORC1 and mTORC2 regulate EMT, motility, and metastasis of colorectal cancer via RhoA and Rac1 signaling pathways. J Transl Med 71 3246. PMID: 21430067.

Dwivedi et al (2010) Rac1-mediated signaling plays a central role in secretion-dependent platelet aggregation in human blood stimulated by atherosclerotic plaque. Sci Rep 8 128. PMID: 21134286.

Gomez et al (2010) Tissue geometry patterns epithelial-mesenchymal transition via intercellular mechanotransduction. Nat Methods 110 44. PMID: 20336666.

Rex et al (2009) Different Rho GTPase-dependent signaling pathways initiate sequential steps in the consolidation of long-term potentiation. Dev Biol 186 85. PMID: 19596849.

Brown and Price (2007) Characterization of Salmonella enterica serovar Typhimurium DT104 invasion in an epithelial cell line (IPEC J2) from porcine small intestine. Vet Microbiol 120 328. PMID: 17157450.

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Keywords: NSC 23766, supplier, Selective, inhibitors, inhibits, Rac1-GEF, interaction, antioncogenic, G, Proteins, Small, NSC23766, 1177865-17-6, Tocris Bioscience, G Protein (Small) Inhibitor products

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