Chemical Name: N-(3,5-Dimethylphenyl)-N'-[2-(trifluoromethyl)phenyl]guanidine
Biological Activity1A-116 is a Rac1 inhibitor. Reduces intracellular Rac1-GTP levels and blocks Rac1-P-Rex1 interaction in vitro. Exhibits no effect on GTPase activity of closely related Cdc42. Displays antiproliferative, anti-invasive and pro-apoptotic activity in several cancer cell lines. Exhibits antimetastatic activity in vivo. Also restores antiproliferative effects of Tamoxifen (Cat. No. 6342) in resistant breast cancer cell.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines.
Cardama et al.
Anticancer Agents Med.Chem., 2014;14:840
Pharmacological inhibition of Rac1-PAK1 axis restores tamoxifen sensitivity in human resistant breast cancer cells.
Gonzalez et al.
Cell Signal., 2017;30:154
Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines.
Cabrera et al.
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