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GNE684

GNE684
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GNE684

Catalog No. T11442Cas No. 2438637-64-8
GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1) with average Ki app values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively [1].
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Pack SizePriceAvailabilityQuantity
25 mgInquiry10-14 weeks
50 mgInquiry10-14 weeks
100 mgInquiry10-14 weeks
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Product Introduction

Bioactivity
Description
GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1) with average Ki app values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively [1].
In vitro
GNE684, at a concentration of 20 μM for 20 hours, effectively inhibits RIP1 kinase-driven cell death across various human and mouse cell lines, as evidenced by cell viability assays in L929, Jurkat, and MEF cells. Furthermore, within a timeframe of 0 to 60 minutes, GNE684 disrupts TBZ-induced processes in HT-29 and J774A.1 cells, including RIP1 autophosphorylation, the interaction between RIP1 and RIP3, RIP3 autophosphorylation, and RIP3-mediated phosphorylation of MLKL, at the same concentration without altering conditions. These findings are supported by Western blot analysis, demonstrating GNE684's potent inhibitory effects on key mechanisms contributing to cell death and signaling pathways.
In vivo
GNE684 did not 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 [1]. GNE684 (50mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs) [1]. Animal Model: Nemo fl/fl Villin.creERT2 mice (NEMO IEC-KO) [1] Dosage: 50 mg/kg Administration: Oral administration; twice daily; from days 2–6 treated with tamoxifen Result: Almost completely protected the NEMO-deficient intestines from colitis and ileitis.
Chemical Properties
Molecular Weight432.48
FormulaC23H24N6O3
Cas No.2438637-64-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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