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 76-89 of 89

  • TBK1/IKKε-IN-6
    Cat. No.
    A79476

    TBK1/IKKε-IN-6

    TBK1/IKKε-IN-6 is a selective inhibitor of TBK1 and IKKε, exhibiting IC50 values below 100 nM for both targets. This compound plays a significant role in modulating inflammatory signaling pathways by inhibiting the activation of these kinases. It is particularly useful in research focused on autoimmune diseases, cancer, and viral infections, enabling the exploration of therapeutic strategies targeting the TBK1/IKKε pathway.

    5 mg
    $795.00
    All 1 sizes
  • MRT 68601 hydrochloride
    Cat. No.
    A79477

    MRT 68601 hydrochloride

    MRT 68601 hydrochloride is a potent TBK1 inhibitor, exhibiting an IC50 value of 6 nM. This compound effectively inhibits autophagosome formation in lung cancer cells, making it a valuable tool for research in cancer biology and autophagy regulation. Its selective targeting of TBK1 positions MRT 68601 hydrochloride as a promising candidate for studies related to therapeutic approaches in lung cancer and other diseases involving autophagic processes.

    5 mg
    $365.00
    10 mg
    $595.00
    All 2 sizes
  • (E/Z)-HOIPIN-1
    Cat. No.
    A79478

    (E/Z)-HOIPIN-1

    Synonyms: (E/Z)-JTP-0819958

    (E/Z)-HOIPIN-1 is a selective inhibitor of the linear ubiquitin chain assembly complex (LUBAC), targeting the IκB kinase (IKK) pathway. With an IC50 value greater than 2.8 μM, this compound effectively inhibits LUBAC-mediated NF-κB activation. Its potential applications include studies of inflammatory responses, cancer biology, and the modulation of immune signaling pathways.

    1 mg
    $25.00
    2 mg
    $35.00
    All 9 sizes
  • SAR113945
    Cat. No.
    A79479

    SAR113945

    SAR113945 is a highly potent inhibitor of IKK-β, exhibiting an IC50 value of 0.4 nM. This compound is primarily utilized in research focusing on inflammatory pathways and oncogenic processes. Its efficacy makes it a valuable tool for investigating the role of IKK-β in various disease states, particularly in understanding mechanisms underlying inflammation and cancer progression.

    Out of stock

    All 3 sizes
  • MLN-0415
    Cat. No.
    A79480

    MLN-0415

    MLN-0415 is an inhibitor of IKKβ, a key regulator in the NF-κB signaling pathway. This compound exhibits significant anti-inflammatory activity and is instrumental in researching conditions such as arthritis and other inflammatory diseases. MLN-0415 facilitates the exploration of therapeutic strategies targeting the modulation of inflammatory responses.

    25 mg
    $1,780.00
    50 mg
    $2,280.00
    All 3 sizes
  • (Rac)-PF-184
    Cat. No.
    A79482

    (Rac)-PF-184

    (Rac)-PF-184 is a selective inhibitor of the inhibitor of κB kinase 2 (IKK-2) with an IC50 value of 37 nM. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research into inflammatory signaling pathways. It is suitable for studies investigating the role of IKK-2 in various biological processes and disease models.

    10 mg
    $1,200.00
    All 1 sizes
  • LLVK
    Cat. No.
    A79483

    LLVK

    LLVK is a selective inhibitor of IκB phosphorylation, effectively suppressing the activation of pro-inflammatory pathways. It has been shown to reduce lipopolysaccharide (LPS)-induced production of cytokines such as IL-1β, IL-6, and TNF-α. LLVK holds potential as a valuable reagent for research focusing on inflammatory bowel disease, rheumatoid arthritis, and other conditions characterized by dysregulated inflammatory responses.

    Out of stock

    All 3 sizes
  • 1-Dehydro-[10]-gingerdione
    Cat. No.
    A79484

    1-Dehydro-[10]-gingerdione

    1-Dehydro-[10]-gingerdione functions as a selective inhibitor of IKKβ by targeting its activation loop, leading to the disruption of IKKβ-mediated phosphorylation of IκBα in macrophages stimulated with various agonists. This compound effectively inhibits LPS-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione holds promise for research into NF-κB-related inflammation and autoimmune disorders.

    Out of stock

    All 3 sizes
  • TBK1 ligand 2
    Cat. No.
    A79485

    TBK1 ligand 2

    TBK1 Ligand 2 is a selective inhibitor of TBK1, a kinase involved in cellular stress response and inflammation. This compound facilitates the synthesis of PROTAC TBK1 degrader-2, providing a valuable tool for research into targeted protein degradation and the modulation of TBK1-associated pathways. TBK1 Ligand 2 may aid in the investigation of its roles in various diseases, including cancer and neurodegenerative disorders.

    Out of stock

    All 3 sizes
  • TBK1-IN-2
    Cat. No.
    A79486

    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.

    Out of stock

    All 3 sizes
  • IKK-IN-3
    Cat. No.
    A79488

    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.

    5 mg
    $795.00
    All 1 sizes
  • GTCpFE
    Cat. No.
    A79490

    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.

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

    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.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • PI3K/PIKK-IN-2
    Cat. No.
    A79872

    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).

    Out of stock

    All 3 sizes

Items 76-89 of 89

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