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
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