Art. -Nr.: HY-114332

GNE-8505

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GNE-8505 is an orally active, blood-brain barrier-permeable selective dual leucine zipper kinase (DLK) inhibitor. GNE-8505 has an IC₅₀ of 0.144 μM for pJNK, and EC₅₀ of 0.457 μM for DRG. GNE-8505 inhibits the DLK/JNK pathway, reduces stress-induced c-Jun phosphorylation levels, decreases neuronal death and suppresses axonal degeneration. GNE-8505 reduces phosphorylated c-Jun levels in the retina, spinal cord and brain tissues of mice. GNE-8505 is applicable to research related to Alzheimer's disease and amyotrophic lateral sclerosis (ALS).

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Reinheit: 99.53%
CAS. Nr.: 1620573-48-9
Formel: C₂₁H₂₄F₃N₅O
Molecular Weight:419.44

Speicherung:

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

GNE-8505 Chemical Structure

CAS. Nr.: 1620573-48-9

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

Biologische Aktivität

Beschreibung

Alle MAP3K Isoform-spezifische Produkte anzeigen :

Alle JNK Isoform-spezifische Produkte anzeigen :

In Vivo

GNE-8505 (3-18 mg/kg; p.o.; single administration) rapidly and dose-dependently reduces injury-induced phosphorylated c-Jun levels in the retina of mice, with an in vivo IC₅₀ of 0.98 μM^[2].
Single administration of GNE-8505 (35 mg/kg) significantly reduces the number of phosphorylated c-Jun-positive cells in the spinal cord of SOD1^G93A ALS mice at the middle stage of the disease^[2].

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

Animal Model:

C57BL/6N (SOD1G93A transgenic line, 14-week-old, mid-disease stage)^[2]
Dosage:

35 mg/kg
Administration:

single dose
Result:

Reduced the number of p-c-Jun-positive cells in lumbar spinal cord sections compared to vehicle-treated mice.

Chemical Information

CAS. Nr. 1620573-48-9
Appearance Solid
Molecular Weight 419.44
Formel C₂₁H₂₄F₃N₅O
Color White to off-white
SMILES

FC(F)(F)C1=CC(C2=NN(C([C@@H]3[C@]4([H])[C@@]3([H])CN(C5COC5)C4)=C2)CC6CC6)=CN=C1N
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 (238.41 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

2.3841 mL

11.9207 mL

23.8413 mL

5 mM

0.4768 mL

2.3841 mL

4.7683 mL

10 mM

0.2384 mL

1.1921 mL

2.3841 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

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
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.

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Acar D, et al. Effect of Dual Leucine Zipper Kinase Inhibitor GNE-3511 on Epileptogenesis and Cognitive and Behavioral Changes in a Temporal Lobe Epilepsy Model in Mice. bioRxiv, 2023: 2023.06. 11.544443.

[2]. Le Pichon CE, et al. Loss of dual leucine zipper kinase signaling is protective in animal models of neurodegenerative disease. Sci Transl Med. 2017;9(403):eaag0394. [Content Brief]

[3]. Siu M, et al. JW. Dual Leucine Zipper Kinase Inhibitors for the Treatment of Neurodegeneration. J Med Chem. 2018 Sep 27;61(18):8078-8087. [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	2.3841 mL	11.9207 mL	23.8413 mL	59.6033 mL
	5 mM	0.4768 mL	2.3841 mL	4.7683 mL	11.9207 mL
	10 mM	0.2384 mL	1.1921 mL	2.3841 mL	5.9603 mL
	15 mM	0.1589 mL	0.7947 mL	1.5894 mL	3.9736 mL
	20 mM	0.1192 mL	0.5960 mL	1.1921 mL	2.9802 mL
	25 mM	0.0954 mL	0.4768 mL	0.9537 mL	2.3841 mL
	30 mM	0.0795 mL	0.3974 mL	0.7947 mL	1.9868 mL
	40 mM	0.0596 mL	0.2980 mL	0.5960 mL	1.4901 mL
	50 mM	0.0477 mL	0.2384 mL	0.4768 mL	1.1921 mL
	60 mM	0.0397 mL	0.1987 mL	0.3974 mL	0.9934 mL
	80 mM	0.0298 mL	0.1490 mL	0.2980 mL	0.7450 mL
	100 mM	0.0238 mL	0.1192 mL	0.2384 mL	0.5960 mL

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GNE-8505

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

CNS-Penetrant Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Antidepressant Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle MAP3K Isoform-spezifische Produkte anzeigen

Alle JNK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE-8505

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

CNS-Penetrant Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Antidepressant Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle MAP3K Isoform-spezifische Produkte anzeigen

Alle JNK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GNE-8505 Related Classifications

Art. -Nr.: HY-114332