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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEKK (MAP3K)-DN-1289
DN-1289

Chemical Structure : DN-1289

CAS No.: 3026597-15-6

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DN-1289 (DN1289)

货号: PC-49564Not For Human Use, Lab Use Only.

DN-1289 (DN1289) is a potent, selective and CNS-penetrant dual inhibitor of leucine zipper kinase (DLK, MAP3K12) and leucine zipper-bearing kinase (LZK, MAP3K13) with IC50 of 17 nM and 40 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    DN-1289 (DN1289) is a potent, selective and CNS-penetrant dual inhibitor of leucine zipper kinase (DLK, MAP3K12) and leucine zipper-bearing kinase (LZK, MAP3K13) with IC50 of 17 nM and 40 nM, respectively.
    DN-1289 exhibits EC50 of 88 nM and 711 nM in DLK and LZK phospho c-Jun cellular assays, repectively.
    DN-1289 dose-dependently protected axons and prevented caspase activation with full axon protection at 1 μM and partial effect at 0.1 and 0.3 μM in DRG neurons.
    DN-1289 150 mg/kg (p.o., b.i.d.) significantly attenuated ONC-induced p-c-Jun elevation in the retina in mice.
    DN-1289 (100 mg/kg, 5 days) exhibited neuroprotective effect in the SOD1G93A mouse model, with significant elevation of the p-c-Jun level and increased expression of genes associated with DLK pathway activation in the SOD1G93A spinal cords.

    物理化学性质&存储条件

    分子量 441.391
    分子式 C18H19F4N7O2
    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

    5-(2-((1S,4S)-2-oxa-5-Azabicyclo[2.2.1]heptan-5-yl)-6-(3,3-difluoropyrrolidin-1-yl)pyrimidin-4-yl)-3-(difluoromethoxy)pyrazin-2-amine

    参考文献

    1. Craig RA 2nd, et al. J Med Chem. 2022 Dec 5. doi: 10.1021/acs.jmedchem.2c01056.

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