Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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].
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 | mouse RIP1:189 nM , human RIP1:21 nM , rat RIP1:691 nM |
In vitro | GNE684 (20 μM; 20 hours) potently inhibits RIP1 kinase-driven cell death in multiple 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 Concentration: 20 μM Incubation Time: 20 hours Result: Inhibited RIP1 kinase driven cell death effectively in several human and mouse cell lines. Western Blot Analysis [1] Cell Line: HT-29 cells, J774A.1 cells Concentration: 0 μM, 20 μM Incubation Time: 0 minute, 15 minutes, 60 minutes Result: Disrupted TBZ (2 μM BV6, 20 ng/ml TNF, 20μM zVAD)-induced RIP1 autophosphorylation, interactions between RIP1 and RIP3, RIP3 autophosphorylation, and phosphorylation of MLKL by RIP3. |
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 2 years
( < 1 mg/ml refers to the product slightly soluble or insoluble )
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GNE684 2438637-64-8 Apoptosis TNF GNE-684 Inhibitor inhibitor inhibit