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

IKK

IκB kinase; I kappa B kinase

IKK

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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.

IKK Isoform Specific Products:

IKK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N2270
    Chicanine
    		Inhibitor 99.96%
    Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity.
    Chicanine
  • 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-123929
    PAWI-2
    		Inhibitor 99.29%
    PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model.
    PAWI-2
  • HY-18710
    BMS-066
    		Inhibitor 99.09%
    BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.
    BMS-066
  • HY-111135
    IKK2-IN-3
    		Inhibitor ≥98.0%
    IKK2-IN-3 (Compound 8) is an IKK2 inhibitor with an IC50 of 0.075 μM.
    IKK2-IN-3
  • HY-P1098B
    Ac2-26 ammonium
    		Degrader
    Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model.
    Ac2-26 ammonium
  • HY-W028127
    IKKβ-IN-4
    		Inhibitor 99.94%
    IKKβ-IN-4 (compound 14) is an IkappaB kinase-β ( IKKβ ) inhibitor with IC50 value of 1.9 μM. IKKβ is a key enzyme in the NF-κB signaling pathway and is involved in the development of many diseases.
    IKKβ-IN-4
  • HY-164881
    TBK1 siRNA-3
    		Inhibitor
    TBK1 siRNA-3 is a small interfering RNA (siRNA) targeting TBK1 that has a knockdown effect on TBK1.
    TBK1 siRNA-3
  • 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-162092
    Multi-target Pt
    		Inhibitor
    Multi-target Pt (IV), an antitumor agent, suppresses the IKKβ phosphorylation, IκBα phosphorylation and NF-κB p65 phosphorylation and nuclear translocation, leading to blocked the NF-kB signal pathway.
    Multi-target Pt
  • 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-107592
    ACHP
    		Inhibitor
    ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies.
    ACHP
  • 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
  • HY-145995
    CS12192
    		Inhibitor
    CS12192 is a compound improving survival and weight gain. CS12192 has the potential for the research of graft-versus-host disease (GVHD) (extracted from the patent CN112773802A).
    CS12192
  • HY-146723
    IKKβ-IN-1
    		Inhibitor
    IKKβ-IN-1 is a potent and orally active IkappaB (IKK-β) inhibitor with IC50 of 0.20 μM. IKKβ-IN-1 can reduce PGE2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality.
    IKKβ-IN-1
  • HY-138931
    TBK1/IKKε-IN-6
    		Inhibitor
    TBK1/IKKε-IN-6 (example 110) is a TBK1 and IKKε inhibitor, with IC50 values of <100 nM for both TBK1 and IKKε.
    TBK1/IKKε-IN-6
Cat. No. Product Name / Synonyms Application Reactivity
IKK Isoform Comparison

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