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Submit ReviewGNE 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.
分子量 | 406.48 |
公式 | C22H26N6O2 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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
关键词: 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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