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IκK/IκB

IκK/IκB inhibitors act on the IκB kinase (IKK) complex, which frees nuclear factor kappa B (NF-κB) from IκB. In 1997 a cytokine-responsive IKK was purified, and the complex was shown to contain two catalytic subunits, IKKα and IKKβ. The kinases phosphorylate IκBα, which marks this inhibitor for degradation and frees NF-κB dimers to enter the nucleus. BMS-345541 HCl, described in 2003, binds an allosteric site on IKK and blocks NF-κB-dependent transcription. IKK-16 inhibits IKKβ and the IKK complex, while IMD 0354 and Bay 65-1942 HCl act mainly on IKKβ. BAY 11-7085 is used to block IκBα phosphorylation in cells. BX-795 targets the related TANK-binding kinase 1 (TBK1) and IKKε along with 3-phosphoinositide-dependent protein kinase 1 (PDK1).

Items 76-80 of 80

  • TBK1-IN-2
    Cat. No.
    A79486
    CAS No.
    3075572-35-6

    TBK1-IN-2

    TBK1-IN-2 is a potent inhibitor of TANK-binding kinase 1 (TBK1) with an IC50 of 775 pM. This compound functions by forming stable hydrogen bonds and π-π stacking interactions with TBK1, thereby inhibiting the phosphorylation of interferon regulatory factor 3 (IRF3). TBK1-IN-2 has demonstrated the ability to synergize with tumor necrosis factor (TNF) and interferon-gamma (IFNγ), enhancing immune-mediated tumor cell death. It is a valuable tool for research applications in cancer immunotherapy.

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    Out of stock

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  • IKK-IN-3
    Cat. No.
    A79488
    CAS No.
    615528-53-5

    IKK-IN-3

    IKK-IN-3 is a potent and selective inhibitor of IkappaB kinase 2 (IKK2, also known as IKKβ), exhibiting IC50 values of 19 nM for IKK2 and 400 nM for IKK1 (IKKα). This compound is valuable in research focused on the regulation of the NF-kB signaling pathway, which plays a critical role in inflammation, immune responses, and cancer progression. IKK-IN-3 can be utilized to investigate the therapeutic potential of IKK2 inhibition in various disease models.

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    5 mg
    $795.00
    All 1 sizes
  • GTCpFE
    Cat. No.
    A79490
    CAS No.
    1588866-45-8

    GTCpFE

    GTCpFE is a selective inhibitor of IKKα/β, functioning within the NF-κB signaling pathway. This compound exhibits significant anti-inflammatory properties by preventing the nuclear translocation of the p65 subunit of NF-κB. Additionally, GTCpFE demonstrates targeted anti-cancer stem-like cell activity by impairing mammosphere formation and reducing the CD44+ CD24- immunophenotype associated with aggressive breast cancer. Its dual mechanism positions GTCpFE as a promising agent for both inflammation and cancer research.

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    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • TBK1/IKKε-IN-1
    Cat. No.
    A79491
    CAS No.
    2058264-32-5

    TBK1/IKKε-IN-1

    TBK1/IKKε-IN-1 is a potent dual inhibitor of TBK1 and IKKε, demonstrating IC50 values of less than 100 nM. This compound is valuable for research applications involving the modulation of inflammatory pathways and immune responses. Its inhibition of these kinases provides a tool for studying their roles in various biological processes and disease states, particularly those related to cancer and neuroinflammation.

    In stock View Details
    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • PI3K/PIKK-IN-2
    Cat. No.
    A79872
    CAS No.
    3109464-36-7

    PI3K/PIKK-IN-2

    PI3K/PIKK-IN-2 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) and phosphoinositide-dependent kinase (PIKK) pathways. This compound demonstrates significant biological activity by modulating signaling pathways involved in cell growth, metabolism, and survival. PI3K/PIKK-IN-2 is suitable for use in research applications focused on targeted therapies, including the development of antibody-drug conjugates (ADCs).

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    Out of stock

    All 3 sizes

Items 76-80 of 80

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