GNE-8505 |CAS:1620574-24-4 Probechem Biochemicals

Chemical Structure : GNE-8505

CAS No.: 1620574-24-4

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

货号: 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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5 mg	￥2980	In stock
10 mg	￥4980	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	423.44
分子式	C20H24F3N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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)-

参考文献

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

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

生物&药学活性

物理化学性质&存储条件

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

生物&药学活性

物理化学性质&存储条件

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