A group 2 PAK inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

GNE-2861

Item No. 29458

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-[1-(2-amino-4-pyrimidinyl)-2-[(2-methoxyethyl)amino]-1H-benzimidazol-6-yl]ethynyl]-cyclohexanol
CAS Number
1394121-05-1
Molecular Formula
C22H26N6O2
Formula Weight
406.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 100 mM
SMILES
COCCNC1=NC2=CC=C(C#CC3(O)CCCCC3)C=C2N1C4=NC(N)=NC=C4
InChi Code
InChI=1S/C22H26N6O2/c1-30-14-13-25-21-26-17-6-5-16(7-11-22(29)9-3-2-4-10-22)15-18(17)28(21)19-8-12-24-20(23)27-19/h5-6,8,12,15,29H,2-4,9-10,13-14H2,1H3,(H,25,26)(H2,23,24,27)
InChi Key
RZXMIHOUHYSGJO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $334

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    GNE-2861 is an inhibitor of the group 2 p21-activated kinases (PAKs; IC50s = 7.5, 126, and 36 nM for PAK4, -5, and -6, respectively).1 It is selective for group 2 PAKs over group 1 PAKs (IC50s = 5.42, 0.97, and >10 μM for PAK1, -2, and -3, respectively), as well as JAK3, KHS1, MAP4K4, and MINK1 at 1 μM. GNE-2861 (0.1-50 μM) inhibits cell migration and reduces cell viability of MDA-MB-436 and MCF-10A PIK3CA cells in a concentration-dependent manner. It sensitizes drug-resistant MCF-7/LCC2 breast cancer cells to tamoxifen (Item No. 13258).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Staben, S.T., Feng, J.A., Lyle, K., et al. Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I ½ kinase inhibitors. J. Med. Chem. 57(3), 1033-1045 (2014).

    2. Zhuang, T., Zhu, J., Li, Z., et al. 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(41), 43853-43868 (2015).