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GNE-8505

Chemical Structure : GNE-8505

CAS No.: 1620574-24-4

GNE-8505 (GNE8505;MAP3K12-IN-14)

Catalog No.: PC-60092Not For Human Use, Lab Use Only.

GNE-8505 (GNE8505) is a potent, selective and CNS-penetrant inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with Ki of 3 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GNE-8505 (GNE8505) is a potent, selective and CNS-penetrant inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with Ki of 3 nM.
GNE-8505 displays no significant inhibitory activity against a panel of 220 kinases (<70% inhibition at 1 uM), 42-fold selectivity over homologous mixed lineage kinase LZK based on binding affinity (Kd) values.
GNE-8505 reduces JNK phosphorylation (p-JNK) in HEK293 cells with IC50 of 0.195 uM, reduces p-MKK4 and p-JNK in models of chronic neurodegeneration.
GNE-8505 displays EC50 of 0.574 uM in a high-content in vitro axon degeneration assay.
GNE-8505 (15 or 50 mg/kg PO) reduces p-c-Jun in the PS2APP model of Alzheimer's disease.

Physicochemical Properties

M.Wt 423.44
Formula C20H24F3N5O2
CAS No. 1620574-24-4
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name

2-Pyridinamine, 5-[1-(1-methylethyl)-5-[(1α,5α,6α)-3-(3-oxetanyl)-3-azabicyclo[3.1.0]hex-6-yl]-1H-pyrazol-3-yl]-3-(trifluoromethoxy)-

References

1. Patel S, et al. J Med Chem. 2017 Oct 12;60(19):8083-8102.

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