Selective inhibitor of Rac1-GEF interaction. Prevents Rac1 activation by Rac-specific guanine nucleotide exchange factors (GEFs) TrioN and Tiam1 (IC50
~ 50 μ
M) without affecting Cdc42 or RhoA activation. Inhibits Rac1-mediated cell functions and is reported to reverse tumor cell phenotyes in prostate cancer cells.
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Rational design and characterization of a Rac GTPase-specific small molecule inhibitor.
Gao et al.
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