1. Apoptosis
  2. RIP kinase
  3. GNE684

GNE684 

Cat. No.: HY-128585
Handling Instructions

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.

For research use only. We do not sell to patients.

GNE684 Chemical Structure

GNE684 Chemical Structure

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Description

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 & Target

IC50: 21 nM (human RIP1), 189 nM (mouse RIP1), 691 nM (rat RIP1)[1]

In Vitro

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
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 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]
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.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

432.48

Formula

C₂₃H₂₄N₆O₃

SMILES

COC1=NC=C(N(C)C([[email protected]@H](NC(C2=NN([[email protected]](C3=CC=CC=C3)CC4)C4=N2)=O)CC5)=O)C5=C1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GNE684
Cat. No.:
HY-128585
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GNE684

Cat. No.: HY-128585