GNE684 |
| Catalog No.GC36170 |
GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Kiapp values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2438637-64-8
Sample solution is provided at 25 µL, 10mM.
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GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Kiapp values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively[1]. IC50: 21 nM (human RIP1), 189 nM (mouse RIP1), 691 nM (rat RIP1)[1]
GNE684 (20 μM; 20 hours) inhibits RIP1 kinase driven cell death effectively in several human and mouse cell lines[1].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[1]. Cell Viability Assay[1] Cell Line: L929 cells, Jurkat cells, MEFs
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[1].GNE684 (50mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs)[1]. Animal Model: Nemofl/fl Villin.creERT2 mice (NEMO IEC-KO)[1]
[1]. Patel S, et al. RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases. Cell Death Differ. 2019 May 17.
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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