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 / Safety Data Sheet

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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.

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

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.

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.

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.

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.

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

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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