GNE 2861

Pricing Availability   Qty
Cat.No. 6490 - GNE 2861 | C22H26N6O2 | CAS No. 1394121-05-1
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)
Datasheet
Citations
Reviews
Literature (3)

Biological Activity

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

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.65 100
ethanol 40.65 100

Preparing Stock Solutions

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 will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.46 mL 12.3 mL 24.6 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

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References

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

Citations for GNE 2861

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