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GGTI-286 hydrochloride

Chemical Structure : GGTI-286 hydrochloride

CAS No.: 181141-66-2

GGTI-286 hydrochloride (GGTI286)

Catalog No.: PC-62473Not For Human Use, Lab Use Only.

GGTI-286 hydrochloride is a CAAX peptidomimetic that is a potent, cell-permeable, and selective inhibitor of GGTase I with IC50 of 2 uM, 25-fold more potent than FTI-277.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    GGTI-286 hydrochloride is a CAAX peptidomimetic that is a potent, cell-permeable, and selective inhibitor of GGTase I with IC50 of 2 uM, 25-fold more potent than FTI-277.
    GGTI-286 inhibits processing of the geranylgeranylated protein Rap1A.
    GGTI-286 inhibits oncogenic K-Ras4B stimulation with IC50 of 1 uM.
    GGTI-286 reduces nuclear localization of β-catenin and transcription dependent on β-catenin/T cell factor in mammalian cells.
    GGTI-286 has significant antiproliferative effect in human malignant glioma cells.

    Physicochemical Properties

    M.Wt 466.037
    Formula C23H32ClN3O3S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    methyl (2S)-2-[[4-[[(2R)-2-amino-3-sulfanylpropyl]amino]-2-phenylbenzoyl]amino]-4-methylpentanoate hydrochloride

    References

    1. Lerner EC, et al. J Biol Chem. 1995 Nov 10;270(45):26770-3.

    2. Nishiya N, et al. Chem Biol. 2014 Apr 24;21(4):530-40.

    3. Lerner EC, et al. Oncogene. 1997 Sep;15(11):1283-8.

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