Catalog Number: 3872
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water and to 75 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Additional Information
Licensing Caveats:
Sold for research use only under license from ExonHit Therapeutics S.A.
Background References
  1. RAC1 inhibition targets amyloid precursor protein processing by γ-secretase and decreases Aβ production in vitro and in vivo.
    Desire et al.
    J.Biol.Chem., 2005;280:37516
  2. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of rac family small GTPases.
    Shutes et al.
    J.Biol.Chem., 2007;282:35666
  3. Characterization of EHT1864, a novel small molecule inhibitor of Rac family small GTPases.
    Onesto et al.
    Methods Enzymol., 2008;439:111

The citations listed below are publications that use Tocris products. Selected citations for EHT 1864 include:

10 Citations: Showing 1 - 10
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  1. Unravelling the Mechanism of TrkA-Induced Cell Death by Macropinocytosis in Medulloblastoma Daoy Cells.
    Authors: Li Et al.
    Mol.Cell Biol. 2016;36:2596
  2. Loss of the E3 ubiquitin ligase HACE1 results in enhanced Rac1 signaling contributing to breast cancer progression.
    Authors: Goka and Lippman
    Am J Physiol Lung Cell Mol Physiol 2015;34:5395
  3. Albumin-associated free fatty acids induce macropinocytosis in podocytes.
    Authors: Chung Et al.
    J Clin Invest 2015;125:2307
  4. Rac1 is required for matrix metalloproteinase 13 production by chondrocytes in response to fibronectin fragments.
    Authors: Long Et al.
    Cell Cycle 2013;65:1561
  5. The slow afterhyperpolarization: a target of β1-adrenergic signaling in hippocampus-dependent memory retrieval.
    Authors: Zhang Et al.
    J Neurosci 2013;33:5006
  6. Rac1 pathway mediates stretch response in pulmonary alveolar epithelial cells.
    Authors: Dipaolo Et al.
    Microbiology 2013;305:L141
  7. Novel role for p21-activated kinase 2 in thrombin-induced monocyte migration.
    Authors: Gadepalli Et al.
    Oncogene 2013;288:30815
  8. Inhibition of hepcidin transcription by growth factors.
    Authors: Goodnough Et al.
    Hepatology 2012;56:291
  9. Targeting of Rac GTPases blocks the spread of intact human breast cancer.
    Authors: Katz Et al.
    Oncotarget 2012;3:608
  10. Tannerella forsythia invasion in oral epithelial cells requires phosphoinositide 3-kinase activation and clathrin-mediated endocytosis.
    Authors: Mishima and Sharma
    Arthritis Rheum 2011;157:2382

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