Art. -Nr.: HY-128585

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.

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Reinheit: 99.08%
CAS. Nr.: 2438637-64-8
Formel: C₂₃H₂₄N₆O₃
Molecular Weight:432.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GNE684 Chemical Structure

CAS. Nr.: 2438637-64-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

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]

Alle RIP kinase Isoform-spezifische Produkte anzeigen :

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.

Chemical Information

CAS. Nr. 2438637-64-8
Appearance Solid
Molecular Weight 432.48
Formel C₂₃H₂₄N₆O₃
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (231.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3122 mL

11.5612 mL

23.1225 mL

5 mM

0.4624 mL

2.3122 mL

4.6245 mL

10 mM

0.2312 mL

1.1561 mL

2.3122 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (11.56 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (11.56 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (11.56 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3122 mL	11.5612 mL	23.1225 mL	57.8061 mL
	5 mM	0.4624 mL	2.3122 mL	4.6245 mL	11.5612 mL
	10 mM	0.2312 mL	1.1561 mL	2.3122 mL	5.7806 mL
	15 mM	0.1541 mL	0.7707 mL	1.5415 mL	3.8537 mL
	20 mM	0.1156 mL	0.5781 mL	1.1561 mL	2.8903 mL
	25 mM	0.0925 mL	0.4624 mL	0.9249 mL	2.3122 mL
	30 mM	0.0771 mL	0.3854 mL	0.7707 mL	1.9269 mL
	40 mM	0.0578 mL	0.2890 mL	0.5781 mL	1.4452 mL
	50 mM	0.0462 mL	0.2312 mL	0.4624 mL	1.1561 mL
	60 mM	0.0385 mL	0.1927 mL	0.3854 mL	0.9634 mL
	80 mM	0.0289 mL	0.1445 mL	0.2890 mL	0.7226 mL
	100 mM	0.0231 mL	0.1156 mL	0.2312 mL	0.5781 mL

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GNE684

MCE Bioactive Compound Library

Alle RIP kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE684 Related Classifications

Art. -Nr.: HY-128585