1A-116
Chemical Name: N-(3,5-Dimethylphenyl)-N'-[2-(trifluoromethyl)phenyl]guanidine
Purity: ≥98%
Biological Activity
1A-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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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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.
Oncotarget., 2017;8:98509
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