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GNE684

Chemical Structure : GNE684

CAS No.: 2438637-64-8

GNE684 (GNE-684, GNE 684)

Catalog No.: PC-49126Not For Human Use, Lab Use Only.

GNE684 (GNE 684) is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively.

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    Biological Activity

    GNE684 (GNE 684) is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively.
    GNE684 inhibits necroptotic cell death in human HT-29, rat H9c2, and mouse L929 cells with EC50 of 6.6, 154 and 81 nM, respectively.
    GNE684 inhibitsTNF-driven cell death effectively in several human and mouse cell lines, disrupts TBZ-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3.
    GNE684 inhibits RIP1 kinase driven cell death, GNE684 inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs).
    GNE684 (50 mg/kg, PO, BID) reduces arthritis and skin inflammation of arthritis in paws and joints compared to wild-type mice.

    Physicochemical Properties

    M.Wt 432.484
    Formula C23H24N6O3
    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

    (S)-N-((S)-7-methoxy-1-methyl-2-oxo-2,3,4,5-tetrahydro-1H-pyrido[3,4-b]azepin-3-yl)-5-phenyl-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide

    References

    1. Snahel Patel, et al. Cell Death Differ. 2020 Jan;27(1):161-175.

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