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

IKK

IκB kinase; I kappa B kinase

IKK

Related Products

PDF 0.82 MB

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-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.
    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-173462
    TBK1-IN-2
    		Inhibitor
    TBK1-IN-2 (Compound A1) is a potent TBK1 inhibitor (IC50: 775 pM). TBK1-IN-2 binds to TBK1 through stable hydrogen bonds and π-π stacking, inhibiting IRF3 phosphorylation. TBK1-IN-2 synergizes with TNF/IFNγ to enhance immune-mediated tumor cell death. TBK1-IN-2 can be used in cancer immunotherapy research.
    TBK1-IN-2
  • HY-16561G
    Resveratrol (GMP)
    		Inhibitor
    Resveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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-172620
    LIB3S0280
    		Inhibitor
    LIB3S0280 is a potent TBK1 inhibitor with an IC50 value of 493.9 nM. LIB3S0280 can inhibit TBK1 downstream signaling by decreasing the phosphorylation of IκBα and AKT. LIB3S0280 leads to G2/M arrest and induces apoptosis in pancreatic cancer cells. LIB3S0280 shows significant inhibition against pancreatic cancer cell lines that highly express TBK1 with IC50 values of 6.64-10.98 μM at 96 h. LIB3S0280 has the potential for pancreatic ductal adenocarcinoma (PDAC) research.
    LIB3S0280
  • 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
  • HY-176192
    SMU-14a
    		Inhibitor
    SMU-14a is a TLR3 inhibitor (IC50: 0.18 µM). SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages and downregulates TNF-α in human peripheral blood monocytes. SMU-14a exerts anti-inflammatory effects by reducing the phosphorylation of p65, ERK, and TBK1 through NF-κB, MAPK, and IRF3 signaling pathways, and decreasing serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used in the study of acute hepatitis.
    SMU-14a
  • HY-136392
    IKK-IN-3
    		Inhibitor
    IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively.
    IKK-IN-3
  • HY-114730
    CGA-JK3
    		Inhibitor
    CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells.
    CGA-JK3
  • HY-N0918R
    Desmethoxyyangonin (Standard)
    		Inhibitor
    Desmethoxyyangonin (Standard) is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin (Standard) is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC50: 0.123  µM). Desmethoxyyangonin (Standard) exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin (Standard) induces CYP3A23 expression and leads to skeletal muscle relaxation.
    Desmethoxyyangonin (Standard)
  • HY-164480
    GTCpFE
    		Inhibitor
    GTCpFE inhibits IKKα/β in the NF-κB pathway with anti-inflammatory activities and blocks p65 nuclear entry, which consists of Dimethyl fumarate (DMF) (HY-17363) linked to Aspirin (ASA) (HY-14654). GTCpFE exhibits selective anti-cancer stem-like cell (CSC) activity by reducing mammosphere growth and the CD44+ CD24- immunophenotype. GTCpFE inhibits breast cancer stem cells, an important NFκB- and PGE2-dependent phenotype in aggressive cancers.
    GTCpFE
  • HY-U00457
    TBK1/IKKε-IN-1
    		Inhibitor
    TBK1/IKKε-IN-1 is a dual TBK1 and IKKε inhibitor extracted from patent US20160376283 A1, Compound 274 in Example 60, has IC50s of <100 nM.
    TBK1/IKKε-IN-1
  • HY-13687R
    IKK 16 (Standard)
    		Inhibitor
    IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.
    IKK 16 (Standard)
  • HY-N15496
    Fusaproliferin
    		Inhibitor
    Fusaproliferin is a sesterterpene mycotoxin isolated from Fusarium solani. Fusaproliferin reverse Lipopolysaccharides (HY-D1056) stimulation and the NF-κB and MAPKs signaling pathways contribute to the anti-inflammatory process. Fusaproliferin exhibits affinity for the TLR4 protein with KD values of 28.6 μM. Fusaproliferin shows cytotoxicity against pancreatic cancer cell with rapid and sub-micromolar IC50.
    Fusaproliferin
  • HY-10172R
    IMD-0354 (Standard)
    		Inhibitor
    IMD-0354 (Standard) is the analytical standard of IMD-0354. This product is intended for research and analytical applications. IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
    IMD-0354 (Standard)
  • HY-13802R
    SC-514 (Standard)
    		Inhibitor
    SC-514 (Standard) is the analytical standard of SC-514. This product is intended for research and analytical applications. SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
    SC-514 (Standard)
  • HY-N0547R
    Nomilin (Standard)
    		Inhibitor
    Nomilin (Standard) is the analytical standard of Nomilin. This product is intended for research and analytical applications. Nomilin is a limonoid compound obtained from the extracts of citrus fruits. Nomilin is an anti-obesity and anti-hyperglycemic agent .
    Nomilin (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
IKK Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.