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GNE684

Catalog No. T11442 CAS 2438637-64-8

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].

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GNE684, CAS 2438637-64-8

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Purity: 98%

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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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

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( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Patel S, et al. RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases. Cell Death Differ. 2019 May 17.

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Keywords

GNE684 2438637-64-8 Apoptosis TNF GNE-684 Inhibitor inhibitor inhibit

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