1. Apoptosis
  2. RIP kinase
  3. GNE684

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

CAS No. : 2438637-64-8

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

432.48

Formula

C23H24N6O3

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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GNE684 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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