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-110341
    MRT 68601 hydrochloride
    		Inhibitor
    MRT 68601 hydrochloride is a TBK1 inhibitor with an IC50 value of 6 nM. MRT 68601 hydrochloride inhibits autophagosome formation in lung cancer cells.
    MRT 68601 hydrochloride
  • HY-16561S1
    Resveratrol-13C6
    		Inhibitor
    Resveratrol-13C6 is the 13C-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-<sup>13</sup>C<sub>6</sub>
  • HY-B0808A
    Oxaprozin potassium
    		Inhibitor
    Oxaprozin potassium is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
    Oxaprozin potassium
  • HY-N11085
    Isophysalin A
    		Inhibitor
    Isophysalin A is a physalin with alpha and beta unsaturated ketone components. Isophysalin A binds to GSH and targets multiple cysteine residues on IKKβ. Isophysalin A also inhibits inducible NO synthase (iNOS) and nitric oxide (NO) production, showing anti-inflammatory activity.
    Isophysalin A
  • HY-13018B
    MRT67307 dihydrochloride
    		Inhibitor
    MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.
    MRT67307 dihydrochloride
  • HY-12687R
    Tizoxanide (Standard)
    		Inhibitor
    Tizoxanide (Standard) is the analytical standard of Tizoxanide. This product is intended for research and analytical applications. Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells.
    Tizoxanide (Standard)
  • HY-114573
    TNF-α-IN-19
    TNF-α-IN-19 is an inhibitor of TNFα that can block the interaction between TNFαRI, TRADD, and RIP1, the EC50 values for TNFα, IL-1β, and IL-1β/TNFα are 2.451, 3.792 and 1.54 μM, respectively. TNF-α-IN-19 only inhibits the degradation of IκBα when cells are stimulated by TNFα and not by IL-1β.
    TNF-α-IN-19
  • HY-N1904
    4′-Hydroxywogonin
    		Inhibitor
    4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis.
    4′-Hydroxywogonin
  • HY-N3364
    Lucidone
    		Inhibitor
    Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibits JNK and p38MAPK signals. Lucidone also has inhibitory activity against Dengue virus (DENV) (EC50=25 μM).
    Lucidone
  • HY-136204
    Resveratrol analog 2
    		Inhibitor
    Resveratrol analog 2 is an analog of Resveratrol (HY-16561). Resveratrol is a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties.
    Resveratrol analog 2
  • HY-148206
    DMX-129
    		Inhibitor
    DMX-129 is an ΙΚΚε and TBK-1 inhibitor with IC50 values of <30 nM for both TBK1 and IKKε.
    DMX-129
  • HY-B0808R
    Oxaprozin (Standard)
    		Inhibitor
    Oxaprozin (Standard) is the analytical standard of Oxaprozin. This product is intended for research and analytical applications. Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties.
    Oxaprozin (Standard)
  • HY-107591
    (Rac)-PF-184
    		Inhibitor
    (Rac)-PF-184 is a potent inhibitory factor-κB kinase 2 (IKK-2) inhibitor with an IC50 of 37 nM. (Rac)-PF-184 has anti-inflammatory effects.
    (Rac)-PF-184
  • HY-13295S
    Vinpocetine-d5
    		Inhibitor
    Vinpocetine-d5 is the deuterium labeled Vinpocetine. Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na+ channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders[1][2][3].
    Vinpocetine-d<sub>5</sub>
  • HY-N10768
    1-Dehydro-[10]-gingerdione
    		Inhibitor
    1-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research.
    1-Dehydro-[10]-gingerdione
  • HY-16561G
    Resveratrol (GMP)
    		Inhibitor
    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. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
    Resveratrol (GMP)
  • HY-161329
    NLRP3-IN-32
    		Inhibitor
    NLRP3-IN-32 (compound 7a), a 3, 4-dihydronaphthalene-1(2H)-one derivative, is a potential NLRP3 inflammatory vesicles inhibitor. NLRP3-IN-32 can block the assembly and activation of NLRP3 inflammasome by down-regulating the expression of NLPR3 and apoptosis-associated speck-like protein containing a CARD (ASC), and inhibiting the production of reactive oxygen species (ROS) and other inflammatory mediators. NLRP3-IN-32 inhibits the phosphorylation of IκBα and NF-κB/p65 and the nuclear translocation of p65, thereby inhibiting NF-κB signaling.
    NLRP3-IN-32
  • HY-D0162R
    Malachite green (hemioxalate) (Standard)
    		Inhibitor
    Malachite green hemioxalate (Standard) is the analytical standard of Malachite green hemioxalate (HY-D0162). This product is intended for research and analytical applications. Malachite green hemioxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green hemioxalate has antimicrobial activity, which is attributed to inhibition of intracellular enzymes, intercalation into DNA, and/or interaction with cellular membranes. Malachite green hemioxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green hemioxalate exhibits antitumor activity in vitro and in vivo.
    Malachite green (hemioxalate) (Standard)
  • HY-107591B
    PF-184
    		Inhibitor
    PF-184 is a potent and selective IKK-2 inhibitor (IC50: 37 nM) over rhIKK-1, IKKi, and more than 30 tyrosine and serine/threonine kinases. PF-184 can be used in the research of inflammation, such as asthma and chronic obstructive pulmonary disease.
    PF-184
  • HY-139833
    Anti-inflammatory agent 6
    Anti-inflammatory agent 6 blocks the phosphorylation of I kappa b kinase α/β (IKKα/β), IκBα, and nuclear factor kB p65 (NF-κB p65) which is a key controller of inflammation, thereby showing anti-inflammatory potential.
    Anti-inflammatory agent 6
Cat. No. Product Name / Synonyms Application Reactivity
IKK Isoform Comparison

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