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Submit ReviewGNE 2861
Description: Group II PAK inhibitor; potently inhibits PAK4 and PAK 6
Chemical Name: 1-[2-[1-(2-Amino-4-pyrimidinyl)-2-[(2-methoxyethyl)amino]-1H-benzimidazol-6-yl]ethynyl]cyclohexanol
Purity: ≥98% (HPLC)
Biological Activity for GNE 2861
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 for GNE 2861
| M. Wt | 406.48 |
| Formula | C22H26N6O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1394121-05-1 |
| PubChem ID | 68181954 |
| InChI Key | RZXMIHOUHYSGJO-UHFFFAOYSA-N |
| Smiles | COCCNC1=NC2=CC=C(C=C2N1C3=NC(N)=NC=C3)C#CC4(O)CCCCC4 |
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.
Product Datasheets for GNE 2861
References for GNE 2861
References are publications that support the biological activity of the product.
Zhuang et al (2015) p21-activated kinase group II small compound inhibitor GNE-2861 perturbs estrogen receptor alpha signaling and restores tamoxifen-sensitivity in breast cancer cells. Oncotarget. 6 43853 PMID: 26554417
Staben et al (2014) Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors. J.Med.Chem. 57 1033 PMID: 24432870
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Keywords: GNE 2861, GNE 2861 supplier, GNE2861, PAK, Kinase, p21, activated, kinase, inhibitors, inhibits, group, II, PAK4, PAK5, PAK6, P21-activated, Kinases, 6490, Tocris Bioscience
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