GNE684

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GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean K_i^app 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

CAS No. : 2438637-64-8

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Biological Activity
Purity & Documentation
References
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Description

GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean K_i^app 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]

Cellular Effect

Cell Line	Type	Value	Description	References
H9c2	IC₅₀	154 nM Compound: GNE684; 54	Inhibition of TNF induced necroptosis cell death in rat H9c2 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6 Inhibition of TNF induced necroptosis cell death in rat H9c2 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6	[PMID: 36346971]
HT-29	IC₅₀	6.6 nM Compound: GNE684; 54	Inhibition of TNF induced necroptosis cell death in human HT-29 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6 Inhibition of TNF induced necroptosis cell death in human HT-29 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6	[PMID: 36346971]
L929	IC₅₀	81 nM Compound: GNE684; 54	Inhibition of TNF induced necroptosis cell death in mouse L929 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6 Inhibition of TNF induced necroptosis cell death in mouse L929 cells incubated for 18 to 24 hrs in presence of TNF/zVAD/BV6	[PMID: 36346971]

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:	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

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

Handling Instructions (2659 KB)

References

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

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.

Keywords:

GNE6842438637-64-8GNE 684GNE-684RIP kinaseReceptor-interacting protein kinasesRIPKInhibitorinhibitorinhibit

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