Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
Pack Size | Availability | Price/USD | Quantity |
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25 mg | 10-14 weeks | Inquiry | |
50 mg | 10-14 weeks | Inquiry | |
100 mg | 10-14 weeks | Inquiry |
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]. |
Targets&IC50 | RIP1 (mouse):189 nM , RIP1 (human):21 nM , RIP1 (rat):691 nM |
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. |
Molecular Weight | 432.48 |
Formula | C23H24N6O3 |
CAS No. | 2438637-64-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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