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IκB/IKK

The IκB kinase (IKK) is an enzyme complex that is involved in propagating the cellular response to inflammation.The IκB kinase enzyme complex is part of the upstream NF-κB signal transduction cascade. The IκBα (inhibitor of nuclear factor kappa B) protein inactivates the NF-κB transcription factor by masking the nuclear localization signals (NLS) of NF-κB proteins and keeping them sequestered in an inactive state in the cytoplasm. Specifically, IKK phosphorylates the inhibitory IκBα protein. This phosphorylation results in the dissociation of IκBα from NF-κB. NF-κB, which is now free, migrates into the nucleus and activates the expression of at least 150 genes; some of which are anti-apoptotic.

  • Kurarinone
    T5S099334981-26-5
    Kurarinone, a flavanoid derived from shrub Sophora flavescens,Kurarinone exhibits anti-tumor, estrogenic, and anti-inflammatory activities, it also shows strong inhibitory effect on immune responses. Kurarinone may ameliorate chronic inflammatory skin diseases through the suppression of pathogenic CD4(+) T-cell differentiation and the overall immune response.
    • $39
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  • Allicin
    T3123539-86-6
    Allicin exerts antioxidant, bactericidal, anti-cancer, anti-inflammatory activities, it exerts an inhibitory immunomodulatory effect on intestinal epithelial cells. Allicin could significantly inhibit vascular smooth muscle cells' proliferation and migration induced by insulin, which may be related to the inhibition of the activation of ERK signal path. Allicin is beneficial in reducing blood cholesterol, triglycerides levels and systolic blood pressure in hypercholesterolemic rats, it may beneficially affect two risk factors for atherosclerosis-hyperlipidemia and hypertension.
    • $40
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  • Amlexanox
    T163968302-57-8
    Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.
    • $32
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  • MRT67307 HCl (1190378-57-4(free base))
    T5162
    MRT67307 is a kinase inhibitor of TBK1, MARK1-4, IKKε, and NUAK1 (IC50: 19, 27-52, 160, and 230 nM, respectively).
    • $37
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  • 2-AMINO-5-PHENYL-THIOPHENE-3-CARBOXYLIC
    T89104815-35-4
    2-AMINO-5-PHENYL-THIOPHENE-3-CARBOXYLIC is Inhibitior of IKKβ.
    • $50
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  • JTP 0819958 - HOIPIN-1
    T8951
    JTP-0819958 is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM[1]. JTP-0819958 suppress LUBAC-mediated NF-kB activation in vitro[2].
    • $33
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  • ACHP Hydrochloride
    T10237406209-26-5In house
    ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.
    • $61
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  • Resveratrol
    T1558501-36-0
    Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.
    • $36
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  • Bay 11-7085
    T1934196309-76-9
    Bay 11-7085 can irreversibly inhibit the IκBα phosphorylation induced by TNFα (IC50: 10 μM).
    • $30
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  • BMS-345541
    T6326445430-58-0
    BMS-345541 (IKK Inhibitor III) is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM, respectively.
    • $32
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  • BAY32-5915
    T207701571-30-8
    BAY32-5915 is an inhibitor of IKKalpha.
    • $39
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  • Rosmarinic acid
    T276520283-92-5
    Rosmarinic acid (Labiatenic acid) is widely found in plants and has antioxidant, anti-inflammatory, and antibacterial activities. It inhibits MAO-A, MAO-B, and COMT with IC50 of 50.1, 184.6, and 26.7 μM respectively.
    • $33
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  • Dehydrocostus Lactone
    T2833477-43-0
    Dehydrocostus Lactone ((-)-Dehydrocostus lactone) shows anti-inflammatory, anti-ulcer, immunomodulatory and anti-tumor properties.
    • $39
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  • IMD-0354
    T6141978-62-1
    IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and inhibits IκBα phosphorylation in NF-κB pathway.
    • $40
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  • TPCA-1
    T3049507475-17-4
    TPCA-1 (TPCA1) is an effective and specific IKK-2 inhibitor (IC50: 17.9 nM); shows >22-fold selectivity over IKK-1 and >550-fold selectivity over others kinases and enzymes.
    • $38
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  • Bardoxolone Methyl
    T6165218600-53-4
    Bardoxolone Methyl (TP-155) is a synthetic triterpenoid that acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway with potential anti-tumor and anti-inflammatory activities.
    • $39
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  • SC-514
    T2118354812-17-2
    SC-514 (GK 01140) is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression.
    • $30
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  • CCCP
    T7081555-60-2
    CCCP (Carbonyl Cyanide m-Chlorophenylhydrazone) is an oxidative phosphorylation (OXPHOS) inhibitor and mitochondrial proton carrier uncoupler. CCCP inhibits the activation of STING and its downstream signaling molecules TBK1 and IRF3.
    • $41
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  • BAY 11-7082
    T190219542-67-7
    BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that inhibits TNFα-induced IκBα phosphorylation (IC50=10 μM). BAY 11-7082 is also an inhibitor of the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19 0.96 μM).
    • $43
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  • Kazinol U
    TN43831238116-48-7
    Kazinol U may have therapeutic value in delaying pancreatic β-cell destruction in type 1 diabetes by blocking the NF-κB pathway in pancreatic β-cells reduces cell damage. Kazinol U shows estrogenic activity with ligand-activity of estrogen receptor, transcriptional activity of estrogen -responsive element-reporter genes, it may have beneficial effects in the treatment of menopausal symptoms.
    • $390
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  • Latifolin
    TN442010154-42-4
    Latifolin is a strong DPPH-scavenger, it attenuates inflammatory responses by inhibiting NF-κB activation via Nrf2-mediated heme oxygenase-1 expression. Latifolin displays potent anticarcinogenic phase II marker enzyme, quinone reductase (QR) inducing activity and high chemopreventive indices. Latifolin also shows antifungal activity against white- and brown-rot fungi.
    • $540
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  • Goshonoside F5
    TN416290851-28-8
    Goshonoside F5 has anti-inflammatory activity, it significantly inhibits the pro-inflammatory response induced by LPS, both in vitro and in vivo.
    • $380
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  • Bakkenolide IIIa
    TN3486915289-60-0
    Bakkenolide IIIa has antioxidant, and neuroprotective effects, it protects against cerebral damage by inhibiting AKT and ERK1/2 activation and inactivated NF-κB signaling.
    • $740
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  • TBK1/IKKε-IN-5
    T79511893397-65-3
    TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor(IC50 of 1 nM and 5.6 nM, respectively).
    • $159
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  • Chlojaponilactone B
    TN36351449382-91-5
    Chlojaponilactone B has anti-inflammatory activity, it exhibits pronounced inhibition of nitric oxide (NO) production in lipopolysaccharide (LPS)-induced RAW 264.7 macrophages.
    • $660
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  • 7,8-Didehydrocimigenol
    TN3219150972-72-8
    7,8-Didehydrocimigenol can be used for the treatment of cardiovascular disorders such as atherosclerosis. It upregulates PPAR-γ in EC inhibits NF-kB activity of TNF-α-activated EC which leads to selective inhibition of VCAM-1 expression.
    • $550
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  • Nyasol
    TN468396895-25-9
    Nyasol may have potential to be developed as medicines for the treatment of allergies by inhibiting the activation of mast cells. Nyasol shows anti-inflammatory properties by inhibiting iNOS expression; it also has antifungal activity, it is significantly
    • $1,790
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  • Cudraflavone B
    TN372619275-49-1
    Cudraflavone B has anti-proliferative activity, mouse brain monoamine oxidase (MAO) inhibitory effects, apoptotic actions in human gastric carcinoma cells and mouse melanoma cells, and hepatoprotective activity. It may be a lead for the development of a potential candidate for human oral squamous cell carcinoma cells.
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  • Dehydroglyasperin C
    TN3806199331-35-6
    Dehydroglyasperin C is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C possesses potent antioxidant, cancer chemopreventive, and neuroprotective activities, it has protective effects against chronic diseases
    • $871
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  • Neoechinulin A
    TN463551551-29-2
    Neoechinulin A has anti-inflammatory effect against LPS-stimulated RAW264.7 macrophages through inhibition of the NF-κB and p38 MAPK pathways, it may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regu
    • $620
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  • 2-Methoxystypandrone
    TN277585122-21-0
    2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant
    • $520
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  • Cearoin
    TN361452811-37-7
    Cearoin has anti-inflammatory, and antiallergic activities, it can markedly inhibit inflammatory responses including LPS-induced NO production by suppressing the expression of iNOS mRNA and LPS-induced mRNA expression of TNFα and CCL2. Cearoin induces aut
    • $524
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  • Bisacurone
    TN3517120681-81-4
    Bisacurone has anti-oxidant, anti-inflammatory, and anti-metastatic activities, it may have a protective effect against ethanol-induced liver injury by suppressing hepatic oxidation and inflammation.
    • $5,578
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  • Olivetol
    T3736500-66-3
    Olivetol (5-n-Amylresorcinol) (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses of tetrahydrocannabinol. Olivetol has an antioxidant effect.
    • $49
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  • GSK319347A
    T15558862812-98-4
    GSK319347A is a selective and potent dual inhibitor of TBK1 and IKKε with potential anti-tumor activity and inhibition of IKK2 activity, which can be used in the study of bladder cancer and lung adenocarcinoma.
    • $67
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  • 1-Hydroxy-2,3,5-trimethoxyxanthone
    TN253422804-49-5
    1-Hydroxy-2,3,5-trimethoxyxanthone (HM-1) has vasodilator action ,which involves both an endothelium-dependent mechanism involving NO and an endothelium-independent mechanism by inhibiting Ca(2+) influx through L-type voltage-operated Ca(2+) channels; a minor contribution to the effects of HM-1 may be related to inhibition of the protein kinase C-mediated release of intracellular Ca(2+) stores. HM-1,at the concentration of 1 ug/mL, can effectively inhibit the osteoclast differentiation in a co-culture system with mouse osteoblastic calvarial cells and bone marrow cells; it also can protect mice from the acute lung injury induced by ipopolysaccharide (LPS), which is relative to the increasing of IκB-α protein expression and the suppressing of inducible nitric oxide synthase and cyclooxygenase-Ⅱ protein expression.
    • $1,598
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  • Isophysalin A
    TN43181363398-67-7
    Isophysalin A exhibits anti-inflammatory activitiy, it exhibits conjugating abilities with glutathione and also shows significant nitric oxide (NO) production inhibiting activities.
    • $860
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  • BAY-985
    T104772409479-29-2
    BAY-985 is a potent, selective, and orally active ATP-competitive dual inhibitor of TBK1 and IKKε (IC50s: 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε) with antitumor efficacy.
    • $175
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  • (Rac)-BAY-985
    T126592101925-20-4
    (Rac)-BAY-985 is a potent, ATP-competitive and selective inhibitor of TBK1(IC50 of 1.5 nM),with antitumor efficacy.
    • $2,120
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  • IKK2-IN-4
    T36524354811-10-2
    IKK2-IN-4(IKK2 Inhibitor VI) is a highly potent IKK-2 inhibitor with an IC50 value of 25 nM. IKK2-IN-4 inhibited the production of TNF-α in PBMC induced by LPS.
    • $188
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  • ACHP
    T22021406208-42-2
    ACHP (IKK-2 Inhibitor VIII) is a novel selective and potent IKK inhibitor with inhibitory effects on IKK-α and IKK-β. ACHP has anti-HIV-1 activity and inhibits HIV-1 long terminal repeat (LTR)-driven gene expression through inhibition of NF-κB activation, inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR, and inhibits TNF-α-induced NF-κB (p65) recruitment to the HIV-1 LTR. ACHKP has anti-HIV-1 activity and inhibits TNF-α-induced recruitment of NF-κB (p65) to the HIV-1 LTR.
    • $48
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  • GSK8612
    T55402361659-62-1
    GSK8612 is a highly selective and potent inhibitor of Tank-binding Kinase-1 (TBK1, pIC50: 6.8) .
    • $39
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  • BI605906
    T14567960293-88-3
    BI605906 is an IKKβ inhibitor that inhibits tumor necrosis factor alpha-dependent IkappaB degradation and expression of the pro-inflammatory mediator interleukin-6, which can be used to study inflammatory skin diseases such as psoriasis.
    • $35
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  • IKK-IN-1
    T11633406211-06-1
    IKK-IN-1 is an inhibitor of IKK.
    • $1,110
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  • Bakkenolide A
    T2S060619906-72-0
    Bakkenolide A has antifeedant and growth inhibitory effects on neonate variegated cutworms, it inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related signaling pathways.
    • $116
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  • GS143
    T25465916232-21-8
    GS143 is a selec­tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup­presses NF-κB acti­va­tion and tran­scrip­tion of tar­get genes and does not inhibit proteasome activity. GS143 has anti-asthm
    • $38
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  • Protosappanin A
    TJS1779102036-28-2
    Protosappanin A (PTA) has anti-oxidative/nitrative activities on brain immune and neuroinflammation through regulation of CD14/TLR4-dependent IKK/IκB/NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.
    • $148
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  • Armepavine
    T3775524-20-9
    Armepavine (R-Armepavine) exerted both in vitro and in vivo antifibrotic effects in rats, with inhibition of NF-κB, JunD and C/EBP pathways. It improves experimental autoimmune crescentic glomerulonephritis.
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    • WS3
      T20551421227-52-2
      WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
      • $44
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    • Bay 65-1942 free base
      T10472L600734-02-9
      Bay 65-1942 free base is an inhibitor of ATP-competitive and selective IKKβ.
      • $1,520
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