Chemical Name: 1-[2-[1-(2-Amino-4-pyrimidinyl)-2-[(2-methoxyethyl)amino]-1H-benzimidazol-6-yl]ethynyl]cyclohexanol
Biological ActivityGNE 2861 is an inhibitor of group II p21 activated kinases (PAK; IC50 values are 7.5, 126 and 36 nM for PAK4, PAK5 and PAK6, respectively). Displays selectivity for group II PAK over a panel of 222 kinases. Inhibits tumor cell proliferation, migration and invasion in two breast cancer cell lines. Also sensitizes tamoxifen-resistant breast cancer cell lines to tamoxifen (Cat. No. 6342) via PAK4-dependent regulation of estrogen receptor α (ERα) target gene expression.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
p21-activated kinase group II small compound inhibitor GNE-2861 perturbs estrogen receptor alpha signaling and restores tamoxifen-sensitivity in breast cancer cells.
Zhuang et al.
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.
Staben et al.
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