GNE 2861
Chemical Name: 1-[2-[1-(2-Amino-4-pyrimidinyl)-2-[(2-methoxyethyl)amino]-1H-benzimidazol-6-yl]ethynyl]cyclohexanol
Purity: ≥98%
Biological Activity
GNE 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.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.
Background References
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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.
Oncotarget., 2015;6:43853 -
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.
Staben et al.
J.Med.Chem., 2014;57:1033
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