EHT 1864

Cat. No. 3872

EHT 1864 C25H27F3N2O4S.2HCl [754240-09-0]

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Chemical Name: 5-(5-(7-(Trifluoromethyl)quinolin-4-ylthio)pentyloxy)-2-(morpholinomethyl)-4H-pyran-4-one dihydrochloride

Biological Activity

Inhibitor of Rac family GTPases. Blocks activation by direct binding to Rac1, Rac1b, Rac2 and Rac3 (KD values are 40, 50, 60 and 250 nM respectively). Inhibits Rac, Ras and Tiam-induced growth transformation of NIH-3T3 fibroblasts. Reduces β-amyloid peptide production in vivo.

Licensing Information

Sold for research use only under license from ExonHit Therapeutics S.A.

Technical Data

M.Wt:
581.47
Formula:
C25H27F3N2O4S.2HCl
Solubility:
Soluble to 100 mM in water and to 75 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
754240-09-0

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

Onesto et al (2008) Characterization of EHT1864, a novel small molecule inhibitor of Rac family small GTPases. Methods Enzymol. 439 111. PMID: 18374160.

Shutes et al (2007) Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of rac family small GTPases. J.Biol.Chem. 282 35666. PMID: 17932039.

Desire et al (2005) RAC1 inhibition targets amyloid precursor protein processing by γ-secretase and decreases Aβ production in vitro and in vivo. J.Biol.Chem. 280 37516. PMID: 16150730.

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Citations are publications that use Tocris products. Selected citations for EHT 1864 include:

Li et al (2016) Unravelling the Mechanism of TrkA-Induced Cell Death by Macropinocytosis in Medulloblastoma Daoy Cells. Mol.Cell Biol. 36 2596. PMID: 27503856 .

Chung et al (2015) Albumin-associated free fatty acids induce macropinocytosis in podocytes. J Clin Invest 125 2307. PMID: 25915582.

Goka and Lippman (2015) Loss of the E3 ubiquitin ligase HACE1 results in enhanced Rac1 signaling contributing to breast cancer progression. Am J Physiol Lung Cell Mol Physiol 34 5395. PMID: 25659579.

Dipaolo et al (2013) Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells. Microbiology 305 L141. PMID: 23686855.

Gadepalli et al (2013) Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration. Oncogene 288 30815. PMID: 24025335.

Long et al (2013) Rac1 is required for matrix metalloproteinase 13 production by chondrocytes in response to fibronectin fragments. Cell Cycle 65 1561. PMID: 23460186.

Zhang et al (2013) The slow afterhyperpolarization: a target of β1-adrenergic signaling in hippocampus-dependent memory retrieval. J Neurosci 33 5006. PMID: 23486971.

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

Katz et al (2012) Targeting of Rac GTPases blocks the spread of intact human breast cancer. Oncotarget 3 608. PMID: 22689141.

Mishima and Sharma (2011) Tannerella forsythia invasion in oral epithelial cells requires phosphoinositide 3-kinase activation and clathrin-mediated endocytosis. Arthritis Rheum 157 2382. PMID: 21622527.

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Keywords: EHT 1864, supplier, Rac-GEF, interaction, antioncogenic, G, Proteins, Small, transformation, Rac1, Rac1b, Rac2, Rac3, Ras, Tiam, inhibits, inhibitors, GTPases, EHT1864, Tocris Bioscience, G Protein (Small) Inhibitor products

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Novel inhibitor of Rac family GTPases

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First to launch the potent Rac inhibitor, EHT 1864 - licensed from ExonHit Therapeutics.