1. Signaling Pathways
  2. NF-κB
  3. IKK

IKK

IκB kinase; I kappa B kinase

IKK is a complex composed of three subunits: IKKα, IKKβ, and IKKγ (also called NEMO). The complex is the signal integration hub for NF-κB activation. It integrates signals from all NF-κB activating stimuli to catalyze the phosphorylation of various IκB and NF-κB proteins, as well as of other substrates. The human IKK family has four members, the IKKs IKK-alpha and IKK-beta, and the IKK-related kinases TBK1 and IKK-epsilon.

Two members, IKKα and IKKβ, the so-called canonical members, phosphoryate IκBα, leading to activation of the transcription factor NF-κB, which controls the expression of many immune and inflammatory genes. The IKK-related proteins TBK-1 and IKK-epsilon have a different substrate--IRF3--which regulates a different set of genes, the products of which include Type I interferons. IKKs are a therapeutic target due to their crucial roles in various biological processes, including the immune response, the stress response, and tumor development.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14682
    GSK319347A
    Inhibitor 99.40%
    GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
    GSK319347A
  • HY-105661
    IMD-0560
    Inhibitor 98.73%
    IMD-0560 is a novel IκB kinase β inhibitor.
    IMD-0560
  • HY-136203
    Resveratrol analog 1
    Inhibitor 98.42%
    Resveratrol analog 1 is an analog of Resveratrol (HY-16561), compound 48. Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.
    Resveratrol analog 1
  • HY-107591A
    (Rac)-PF-184 hydrate
    Inhibitor ≥98.0%
    (Rac)-PF-184 hydrate is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 hydrate has anti-inflammatory effects.
    (Rac)-PF-184 hydrate
  • HY-13873
    IKK-IN-1
    Inhibitor
    IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13.
    IKK-IN-1
  • HY-112557
    PROTAC TBK1 degrader-2
    Inhibitor 98.20%
    PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM).
    PROTAC TBK1 degrader-2
  • HY-19362
    AZD3264
    Inhibitor 99.46%
    AZD3264 is a selective IkB-kinase IKK2 inhibitor.
    AZD3264
  • HY-14180
    PHA 408
    Inhibitor ≥98.0%
    PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation.
    PHA 408
  • HY-15473A
    MLN120B dihydrochloride
    Inhibitor 99.73%
    MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
    MLN120B dihydrochloride
  • HY-13018A
    MRT67307 hydrochloride
    Inhibitor
    MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells.
    MRT67307 hydrochloride
  • HY-112456
    IKK2-IN-4
    Inhibitor 99.36%
    IKK2-IN-4 (compound 4) is a potent IKK-2 inhibitor, with an IC50 of 25 nM. IKK2-IN-4 can inhibit the LPS-induced production of TNFα in PBMCs.
    IKK2-IN-4
  • HY-16561S
    Resveratrol-d4
    Inhibitor ≥98.0%
    Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
    Resveratrol-d<sub>4</sub>
  • HY-136741
    BOT-64
    Inhibitor 99.77%
    BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription.
    BOT-64
  • HY-50949
    Bay 65-1942 free base
    Inhibitor
    Bay 65-1942 free base is an ATP-competitive and selective IKKβ inhibitor.
    Bay 65-1942 free base
  • HY-50949A
    Bay 65-1942 (R form)
    Inhibitor
    Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.
    Bay 65-1942 (R form)
  • HY-B0788
    LY2409881
    Inhibitor
    LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.
    LY2409881
  • HY-107593
    PS-1145 dihydrochloride
    Inhibitor
    PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats.
    PS-1145 dihydrochloride
  • HY-133117A
    (Rac)-BAY-985
    Inhibitor
    (Rac)-BAY-985 (Compound Example 100.01) is a potent, ATP-competitive and selective TBK1 inhibitor with an IC50 of 1.5 nM. Antitumor efficacy.
    (Rac)-BAY-985
  • HY-136393
    IKK-IN-4
    Inhibitor
    IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively.
    IKK-IN-4
  • HY-163412
    IKKβ-IN-3
    Inhibitor
    IKKβ-IN-3 (Compound hit4) is a IKKβ inhibitor with an IC50 value of 30.4 nM. IKKβ is a key enzyme in the NF-κB signaling pathway and is involved in the development of many diseases. IKKβ-IN-3 can be used in the study of CAF-induced arthritis.
    IKKβ-IN-3
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