GNE684 |
| Katalog-Nr.GC36170 |
GNE684 ist ein potenter Inhibitor des potenten Rezeptor-interagierenden Proteins 1 (RIP1) mit mittleren Kiapp-Werten von 21 nM, 189 nM und 691 nM fÜr menschliches Maus- bzw. Ratten-RIP1.
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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