GNE 2861

Key Product Details

Product Description

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.

Product Specifications for GNE 2861

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for GNE 2861

The following data is based on the product molecular weight 406.48.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.46 mL	12.30 mL	24.60 mL
5 mM	0.49 mL	2.46 mL	4.92 mL
10 mM	0.25 mL	1.23 mL	2.46 mL
50 mM	0.05 mL	0.25 mL	0.49 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Staben Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors. J.Med.Chem. 2014 PMID: 24432870
• Zhuang p21-activated kinase group II small compound inhibitor GNE-2861 perturbs estrogen receptor alpha signaling and restores tamoxifen-sensitivity in breast cancer cells. Oncotarget. 2015 PMID: 26554417

Product Documents for GNE 2861