GNE 2861

Discontinued Product

6490 has been discontinued.

View all P21-activated Kinases products.
说明: Group II PAK inhibitor; potently inhibits PAK4 and PAK 6
化学名: 1-[2-[1-(2-Amino-4-pyrimidinyl)-2-[(2-methoxyethyl)amino]-1H-benzimidazol-6-yl]ethynyl]cyclohexanol
纯度: ≥98% (HPLC)
说明书
引用文献
评论

生物活性 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.

技术数据 for GNE 2861

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 for GNE 2861

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

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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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