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首页-小分子抑制剂&激动剂-Apoptosis-RIP kinase-GNE684
GNE684

Chemical Structure : GNE684

CAS No.: 2438637-64-8

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GNE684 (GNE-684, GNE 684)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 432.484
    分子式 C23H24N6O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    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

    参考文献

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

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