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GNE684
Catalog No. T11442Cas No. 2438637-64-8
GNE684 is a potent inhibitor of receptor interacting protein 1 (RIP1) with average Ki app values of 21 nM for human, 189 nM for mouse, and 691 nM for rat RIP1, respectively [1].
GNE684
Catalog No. T11442Cas No. 2438637-64-8
GNE684 is a potent inhibitor of receptor interacting protein 1 (RIP1) with average Ki app values of 21 nM for human, 189 nM for mouse, and 691 nM for rat RIP1, respectively [1].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | Inquiry | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | |
| 100 mg | Inquiry | 10-14 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| Description | GNE684 is a potent inhibitor of receptor interacting protein 1 (RIP1) with average Ki app values of 21 nM for human, 189 nM for mouse, and 691 nM for rat RIP1, respectively [1]. |
| Targets&IC50 | RIP1 (human):21 nM , RIP1 (rat):691 nM , RIP1 (mouse):189 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 affect overall survival or tumor growth in the KPP or KPR (LSL-Kras G12D/+; p16/p19 fl/wt; Trp53 R270H/wt; Pdx1-cre) PDAC models. However, GNE684 (50 mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs) [1]. In the Nemo fl/fl Villin.creERT2 mice (NEMO IEC-KO) model, oral administration of 50 mg/kg twice daily from days 2–6 with tamoxifen almost completely protected the NEMO-deficient intestines from colitis and ileitis. |
| Molecular Weight | 432.48 |
| Formula | C23H24N6O3 |
| Cas No. | 2438637-64-8 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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