BiochemProbe — Life Science Research Reagents

GNE-8505 free base · Synonyms: GNE 8505 · GNE8505

GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase.

For research use only. Not for human or veterinary use.

Purity >98% Stock Inquire

GNE-8505 structure

CAS No.: 1620573-48-9

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
10 mg USD 420.00 BP-01907-10mg In stock Get quote
25 mg USD 650.00 BP-01907-25mg In stock Get quote
50 mg USD 920.00 BP-01907-50mg In stock Get quote
100 mg USD 1,320.00 BP-01907-100mg In stock Get quote
250 mg USD 2,120.00 BP-01907-250mg In stock Get quote
500 mg Inquire BP-01907-500mg In stock Inquire
1 g Inquire BP-01907-1g Inquire Inquire

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Description

GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK) .

Biological activity

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. 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.

Identifiers

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
InChIKey
IRPVABHDSJVBNZ-QWHZDKJVSA-N

Specifications

MW (average)
419.4434
Formula
C21H24F3N5O
CAS No.
1620573-48-9
Physical state
Solid
Color
white to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder   -20°C, 3 years , 4°C, 2 years ; In solvent    -20°C, 1 month

Solubility

Soluble in DMSO : 100 mg/mL

References

[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.
[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.

Same target

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Same research area

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