GNE684,2438637-64-8

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GNE684

CAS No. : 2438637-64-8

MCE 国际站：GNE684

产品活性：GNE684 是一种有效的受体相互作用蛋白 1 (RIP1) 抑制剂，作用于人类、小鼠与大鼠 RIP1 的 K_i^app 值分别为 21 nM、189 nM 和 691 nM。

研究领域：Apoptosis

作用靶点：RIP kinase

In Vitro: GNE684 (20 μM; 20 hours) inhibits RIP1 kinase driven cell death effectively in several human and mouse cell lines.
GNE684 (20 μM; 0-60 minutes) disrupts TBZ (2 μM BV6, 20 ng/ml TNF, 20 μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3.

In Vivo: GNE684 also had no impact on overall survival or tumor growth in the KPP or KPR (LSL-Kras ^G12D/+; p16/p19 ^fl/wt ; Trp53 ^R270H/wt ; Pdx1-cre) PDAC models.
GNE684 (50mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs).

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