2. MAPK/ERK Pathway
  3. MAP3K JNK
  4. GNE-8505

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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GNE-8505

GNE-8505 Chemische Struktur

CAS. Nr. : 1620573-48-9

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10 mM * 1 mL in DMSO
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GNE-8505 Related Antibodies

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Alle MAP3K Isoform-spezifische Produkte anzeigen:

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MAP3K7/TAK1 MAP3K8/COT/Tpl2 MAP3K6/ASK2 MAP3K5/ASK1 MAP3K12/DLK/Pref-1 NIK/MAP3K14

Alle JNK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
JNK1 JNK2 JNK3 JNK

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Beschreibung

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)[1][2][3].

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 SOD1G93A 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.
Molekulargewicht

419.44

Formel

C21H24F3N5O
CAS. Nr.
Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3841 mL 11.9207 mL 23.8413 mL
5 mM 0.4768 mL 2.3841 mL 4.7683 mL
View the Complete Stock Solution Preparation Table

* 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

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

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Reinheit & Dokumentation

Purity: 99.53%

SDS (251 KB)

COA (249 KB) HNMR (261 KB) LCMS (331 KB)

Handling Instructions (2659 KB)
Verweise

Complete Stock Solution Preparation Table

* 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.

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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  • 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:

GNE-85051620573-48-9GNE8505GNE 8505MAP3KJNKMAP kinase kinase kinase, MEKK, MAPKKKc-Jun N-terminal kinaseaxon degenerationc-Jun phosphorylationDLK/MAP3K12SOD1G93A ALS micedual leucine zipper kinaseneuron deathmouse retinaALSDLK/JNK pathwaymouse spinal cordsamyotrophic lateral sclerosismouse brainsAlzheimer's diseaseInhibitorinhibitorinhibit

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