1620573-48-9
Chemical Structure
GNE-8505
- CAS No.: 1620573-48-9
- Formula:C21H24F3N5O
- Molecular Weight:419.44
IUPAC Name: 5-(1-(cyclopropylmethyl)-5-((1R,5S,6r)-3-(oxetan-3-yl)-3-azabicyclo[3.1.0]hexan-6-yl)-1H-pyrazol-3-yl)-3-(trifluoromethyl)pyridin-2-amine
InChIKey: IRPVABHDSJVBNZ-QWHZDKJVSA-N
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
Biological Activity: 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].
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GNE-8505 | 99.53% | 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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- [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]
Keywords
