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首页-小分子抑制剂&激动剂-NF-κB Pathway-NF-κB inducing Kinase (NIK)-NIKinh
NIKinh

Chemical Structure : NIKinh

CAS No.: 924143-41-9

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NIKinh (NIK inh)

货号: PC-73055Not For Human Use, Lab Use Only.

NIKinh (NIK inhibitor) is a highly specific, potent NF-κB-inducing kinase (NIK) inhibitor with IC50 of 5.12 uM in ADP-Glo assay.

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

    生物&药学活性

    NIKinh (NIK inhibitor) is a highly specific, potent NF-κB-inducing kinase (NIK) inhibitor with IC50 of 5.12 uM in ADP-Glo assay.
    NIKin hinhibits NIK's ability to phosphorylate a substrate protein in vitro in an ATP-dependent manner (ADP-Glo assay).
    NIKinh also reduced EZH2 expression, a downstream target of NIK, in a dose-dependent manner in a melanoma cell line characterized by upregulation of non-canonical pathway (A375), and concomitantly increased the expression of CDKN1A/p21.
    NIKinh decreased cleavage of p100 into p52, and EZH2 at the protein level in A375 cells, lung cancer cells (A549), and freshly isolated patient melanoma cells (C12.06).
    NIKinh single treatment and combined with anti-PD-1 resulted in significantly increased survival of up to 60% and 70% of the plck-GAPDH tumor-engrafted mice, respectively.
    NIKinh treatment ex vivo reduced the growth of CD4+ Tfh cells from hAITL biopsies upon TCR stimulation, whereas healthy CD4+ T cells remained unaffected.

    物理化学性质&存储条件

    分子量 314.769
    分子式 C17H15ClN2O2
    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

    7-chloro-N-(3,4-dimethoxyphenyl)quinolin-4-amine

    参考文献

    1. Mondragón L, et al. Cancer Cell. 2019 Sep 16;36(3):268-287.e10.

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