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Submit ReviewNSC 23766
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% (HPLC)
Biological Activity for NSC 23766
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.
Compound Libraries for NSC 23766
NSC 23766 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for NSC 23766
| M. Wt | 530.97 |
| Formula | C24H35N7.3HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1177865-17-6 |
| PubChem ID | 16759159 |
| InChI Key | CPUHORIUXPQCHW-UHFFFAOYSA-N |
| Smiles | Cl.Cl.Cl.CCN(CC)CCCC(C)NC1=NC(C)=CC(NC2=CC=C3N=C(C)C=C(N)C3=C2)=N1 |
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.
Solubility Data for NSC 23766
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 53.1 | 100 | |
| DMSO | 53.1 | 100 |
Preparing Stock Solutions for NSC 23766
The following data is based on the product molecular weight 530.97. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.88 mL | 9.42 mL | 18.83 mL |
| 5 mM | 0.38 mL | 1.88 mL | 3.77 mL |
| 10 mM | 0.19 mL | 0.94 mL | 1.88 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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Product Datasheets for NSC 23766
References for NSC 23766
References are publications that support the biological activity of the product.
Gao et al (2004) Rational design and characterization of a Rac GTPase-specific small molecule inhibitor. Proc.Natl.Acad.Sci.USA 101 7618 PMID: 15128949
Floerchinger et al (2021) Optimizing metastatic-cascade-dependent Rac1 targeting in breast cancer: Guidance using optical window intravital FRET imaging. Cell Rep. 36 109689 PMID: 34525350
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Keywords: NSC 23766, NSC 23766 supplier, Selective, inhibitors, inhibits, Rac1-GEF, interaction, antioncogenic, G, Proteins, Small, NSC23766, 1177865-17-6, Rho, 2161, Tocris Bioscience
56 Citations for NSC 23766
Citations are publications that use Tocris products. Selected citations for NSC 23766 include:
Abedini et al (2016) WNT5a is required for normal ovarian follicle development and antagonizes g.tropin responsiveness in granulosa cells by suppressing canonical WNT signaling. FASEB J 30 1534 PMID: 26667040
Chang et al (2016) 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. Virulence 7 806 PMID: 27221788
Prowse et al (2013) Inhibition of Rac and ROCK signalling influence osteoblast adhesion, differentiation and mineralization on titanium topographies. PLoS One 8 e58898 PMID: 23505566
Tabdili et al (2012) Cadherin point mutations alter cell sorting and modulate GTPase signaling. J Cell Sci 125 3299 PMID: 22505612
Goodnough et al (2012) Inhibition of hepcidin transcription by growth factors. Hepatology 56 291 PMID: 22278715
Tang et al (2012) ROCK1 feedback regulation of the upstream small GTPase RhoA. Cell Signal 24 1375 PMID: 22430126
McHenry et al (2010) P190B RhoGAP has pro-tumorigenic functions during MMTV-Neu mammary tumorigenesis and metastasis. Breast Cancer Res 12 R73 PMID: 20860838
Lionarons et al (2019) RAC1P29S Induces a Mesenchymal Phenotypic Switch via Serum Response Factor to Promote Melanoma Development and Therapy Resistance. Cancer Cell 36 68 PMID: 31257073
Cosgrove (2016) N-cadherin adhesive interactions modulate matrix mechanosensing and fate commitment of mesenchymal stem cells. Nature Materials 15 1297 PMID: 27525568
Lichius et al (2014) CDC-42 and RAC-1 regulate opposite chemotropisms in Neurospora crassa. J Cell Sci 127 1953 PMID: 24790223
Gomez et al (2010) Tissue geometry patterns epithelial-mesenchymal transition via intercellular mechanotransduction. Nat Methods 110 44 PMID: 20336666
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
Yao et al (2015) Endothelial Rac1 is essential for hematogenous metastasis to the lung. Sci Rep 6 17501 PMID: 25991673
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
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
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
Yevick et al (2015) Architecture and migration of an epithelium on a cylindrical wire. Nat Commun 112 5944 PMID: 25922533
Tseng et al (2012) Magnetic nanoparticle-mediated massively parallel mechanical modulation of single-cell behavior. Oncotarget 9 1113 PMID: 23064517
Akhmetshina et al (2012) Activation of canonical Wnt signalling is required for TGF-β-mediated fibrosis. Biomol Ther (Seoul) 3 735 PMID: 22415826
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
Hou et al (2014) The Rac1 inhibitor NSC23766 suppresses CREB signaling by targeting NMDA receptor function. J Neurosci 34 14006 PMID: 25319697
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
Huttunen et al (2014) Coxsackievirus A9 infects cells via nonacidic multivesicular bodies. J Virol 88 5138 PMID: 24574401
Hergueta-Redondo et al (2014) Gasdermin-B promotes invasion and metastasis in breast cancer cells. PLoS One 9 e90099 PMID: 24675552
Kenny et al (2014) Mesothelial cells promote early ovarian cancer metastasis through fibronectin secretion. J Clin Invest 124 4614 PMID: 25202979
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
Serra et al (2015) SimV. Increases Fibulin-2 Expression in Human Coronary Artery Smooth Muscle Cells via RhoA/Rho-Kinase Signaling Pathway Inhibition. PLoS One 10 e0133875 PMID: 26207907
Grönholm et al (2011) TCR-induced activation of LFA-1 involves signaling through Tiam1. J Immunol 187 3613 PMID: 21876037
Chun and Shim (2015) EP2 Induces p38 Phosphorylation via the Activation of Src in HEK 293 Cells. Oncotarget 23 539 PMID: 26535079
Wang et al (2015) Inhibition of prostate smooth muscle contraction and prostate stromal cell growth by the inhibitors of Rac, NSC23766 and EHT1864. Br J Pharmacol 172 2905 PMID: 25631101
Tsuchiya et al (2015) Rac1 and ROCK are implicated in the cell surface delivery of GLUT4 under the control of the Ins signal mimetic diDCP-LA-PE. J Pharmacol Sci 128 179 PMID: 26238253
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
Uotila et al (2014) Specific phosphorylations transmit signals from leukocyte β2 to β1 integrins and regulate adhesion. J Cell Biol 289 32230 PMID: 25278023
Fort et al (2011) Activity of the RhoU/Wrch1 GTPase is critical for cranial neural crest cell migration. Dev Biol 350 451 PMID: 21156169
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
Wu et al (2018) Bladder cancer extracellular vesicles drive tumorigenesis by inducing the unfolded protein response in endoplasmic reticulum of non-malignant cells. J Biol Chem PMID: 30593508
Wisdom et al (2018) Matrix mechanical plasticity regulates cancer cell migration through confining microenvironments. Nat Commun 9 4144 PMID: 30297715
Freudenblum et al (2018) In vivo imaging of emerging endocrine cells reveals a requirement for PI3K-regulated motility in pancreatic islet morphogenesis. Development 145 PMID: 29386244
Ford et al (2018) Chlamydia exploits filopodial capture and a macropinocytosis-like pathway for host cell entry. PLoS Pathog 14 e1007051 PMID: 29727463
Gibon et al (2015) proBDNF and p75NTR Control Excitability and Persistent Firing of Cortical Pyramidal Neurons. J Neurosci 35 9741 PMID: 26134656
Kassmer et al (2015) Migration of germline progenitor cells is directed by sphingosine-1-phosphate signalling in a basal chordate. Nat Commun 6 8565 PMID: 26456232
Lomakin et al (2015) Competition for actin between two distinct F-actin networks defines a bistable switch for cell polarization. Nat Cell Biol 17 1435 PMID: 26414403
Cabet et al (2015) Antioxidant Treatment and Induction of Autophagy Cooperate to Reduce Desmin Aggregation in a Cellular Model of Desminopathy. PLoS One 10 e0137009 PMID: 26333167
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
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
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
Martin et al (2013) Pak and Rac GTPases promote oncogenic KIT-induced neoplasms. J Clin Invest 123 4449 PMID: 24091327
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
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
Moore et al (2013) Par3 controls neural crest migration by promoting microtubule catastrophe during contact inhibition of locomotion. Development 140 4763 PMID: 24173803
Eum et al (2009) NADPH oxidase and lipid raft-associated redox signaling are required for PCB153-induced upregulation of cell adhesion molecules in human brain endothelial cells. Toxicol Appl Pharmacol 240 299 PMID: 19632255
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
Carvalho et al (2019) Non-canonical Wnt signaling regulates junctional mechanocoupling during angiogenic collective cell migration. Elife 8 PMID: 31246175
Chang et al (2017) Paxillin facilitates timely neurite initiation on soft-substrate environments by interacting with the endocytic machinery. Elife 6 PMID: 29271742
Benedicto (2017) Concerted regulation of retinal pigment epithelium basement membrane and barrier function by angiocrine factors. Nat Commun 8 15374 PMID: 28524846
Wang et al (2017) The Small GTPase Rac1 Contributes to Extinction of Aversive Memories of Drug Withdrawal by Facilitating GABAA Receptor Endocytosis in the vmPFC. J Neurosci 37 7096 PMID: 28630256
Do you know of a great paper that uses NSC 23766 from Tocris? Please let us know.
Reviews for NSC 23766
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Filter by:
Specific rac inhibitor.
By
Anonymous on 03/26/2018
Assay Type: In Vitro
Species: Other
Rac specific inhibitor
