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
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RAC1 inhibition targets amyloid precursor protein processing by γ-secretase and decreases Aβ production in vitro and in vivo.
Desire et al.
Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of rac family small GTPases.
Shutes et al.
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:
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