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NIKinh

Chemical Structure : NIKinh

CAS No.: 924143-41-9

NIKinh (NIK inh)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 314.769
    Formula C17H15ClN2O2
    Appearance Solid
    CAS No.
    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/SMILES

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

    References

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

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