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-114454
    INH14
    		Inhibitor ≥98.0%
    INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
    INH14
  • HY-124652
    TBK1/IKKε-IN-4
    		Inhibitor 99.42%
    TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR.
    TBK1/IKKε-IN-4
  • HY-160477
    DC-SX029
    		Inhibitor 98.07%
    DC-SX029 is a potent SNX10 protein-protein interaction (PPI) inhibitor with oral activity with an estimated KD constant of ~0.935 μM by surface plasmon resonance (SPR). DC-SX029 blocks the SNX10-PIKfyve interaction, thereby decreased the TBK1/c-Rel signaling activation. DC-SX029 does not affect the protein level of SNX10. DC-SX029 has the potential for inflammatory bowel disease (IBD) research.
    DC-SX029
  • HY-D0162
    Malachite green hemioxalate
    		Inhibitor ≥98.0%
    Malachite green hemioxalate (MCCK1) is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green hemioxalate has antibacterial activity, which is attributed to inhibition of intracellular enzymes, insertion into DNA and/or interaction with cell 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
  • 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-135366
    HPN-01
    		Inhibitor 98.61%
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.
    HPN-01
  • HY-14682
    GSK319347A
    		Inhibitor 99.25%
    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-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-16561S
    Resveratrol-d4
    		Inhibitor 99.36%
    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-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-123936
    SR12343
    		Inhibitor 98.30%
    SR12343, an IKK/NF-κB inhibitor, is a NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic. SR12343 inhibits TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, with an IC50 of 37.02 μM for TNF-α-mediated NF-κB activation. SR12343 suppresses LPS-induced acute pulmonary inflammation in mice. SR12343 can be used for research of inflammatory and degenerative diseases.
    SR12343
  • 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-105661
    IMD-0560
    		Inhibitor 98.73%
    IMD-0560 is a novel IκB kinase β inhibitor.
    IMD-0560
  • HY-19362
    AZD3264
    		Inhibitor 99.46%
    AZD3264 is a selective IkB-kinase IKK2 inhibitor.
    AZD3264
  • 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-169053
    SU1261
    		Inhibitor 99.13%
    SU1261 is an IKK inhibitor with Ki values of 10 nM and 680 nM for IKKα and IKKβ, respectively. SU1261 can inhibit non-canonical NF-κB signaling in U2OS osteosarcoma cells.
    SU1261
  • HY-112456
    IKK2-IN-4
    		Inhibitor 99.89%
    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-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-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-12383
    Pelubiprofen
    		Inhibitor 99.27%
    Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC50 values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.
    Pelubiprofen
Cat. No. Product Name / Synonyms Application Reactivity
IKK Isoform Comparison

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